947 results match your criteria efficient diastereoselective

Diversity-Oriented Synthesis of Spiropyrrolo[1,2-]isoquinoline Derivatives via Diastereoselective and Regiodivergent Three-Component 1,3-Dipolar Cycloaddition Reactions: and Evaluation of the Antidiabetic Activity of Rhodanine Analogues.

J Org Chem 2021 Sep 21. Epub 2021 Sep 21.

Institut UTINAM - UMR CNRS 6213, Université Bourgogne Franche-Comté, 16 Route de Gray, 25030 Besançon, France.

An efficient diastereoselective route is developed to get access to novel spiropyrrolo[1,2-]isoquinoline-oxindole skeletons by a -component [3 + 2] cycloaddition reaction of ()-5-arylidene-1,3-thiazolidine-2,4-diones, isatin derivatives, and 1,2,3,4-tetrahydroisoquinoline (THIQ). Interestingly, the regioselectivity of the reaction is both temperature- and solvent-dependent, allowing the synthesis of two regioisomeric -dispiropyrrolo[2,1-]isoquinolineoxindoles in excellent yield. Unprecedentedly, each isomeric dispiropyrrolo[2,1-]isoquinolineoxindole endured 1,3-dipolar cycloaddition/recycloaddition reactions under thermal or catalytic conditions to regenerate the corresponding regioisomeric counterpart. Read More

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September 2021

O2-Assisted Four-component Reaction of Vinyl Magnesium Bromide with Chiral N-tert-Butanesulfinyl Imines To Form syn-1, 3-Amino Alcohols.

Angew Chem Int Ed Engl 2021 Sep 14. Epub 2021 Sep 14.

Sichuan University, West China School of Pharmacy, CHINA.

An O 2 -assisted, four-component reaction has been developed to synthesize a wide range of syn -1,3-amino alcohols in one step. The reaction proceeds by oxygenation of vinyl magnesium bromide ( component-I ) with O 2 ( component-II ) to give a magnesium enolate of acetaldehyde, which undergoes addition to a chiral N - tert -butanesulfinyl imine ( component-III ) followed by a sequential addition with excess vinyl magnesium bromide ( component-IV ). The approach allows diastereoselective synthesis of anti / syn - and syn / syn -3-amino-1,5-diols in good yields with high diastereoselectivity. Read More

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September 2021

Stereoselective Late-Stage Transformations of Indolo[2,3-]quinolizines Skeleta to Nature-Inspired Scaffolds.

J Org Chem 2021 Sep 3;86(18):12872-12885. Epub 2021 Sep 3.

Sharjah Institute for Medical Research, University of Sharjah, P.O. Box 27272, Sharjah 00000, UAE.

The indolo[2,3-]quinolizines, canthines, and arborescidines natural products exhibit a wide range of bioactivities including anticancer, antiviral, antibacterial, and anti-inflammatory, among others. Therefore, the development of modular and efficient strategies to access the core scaffolds of these classes of natural products is a remarkable achievement. The Complexity-to-Diversity (CtD) strategy has become a powerful tool that transforms natural products into skeletal and stereochemical diversity. Read More

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September 2021

Facile generation of bridged medium-sized polycyclic systems by rhodium-catalysed intramolecular (3+2) dipolar cycloadditions.

Nat Commun 2021 09 2;12(1):5239. Epub 2021 Sep 2.

Shenzhen Grubbs Institute, Department of Chemistry, Southern University of Science and Technology, Shenzhen, China.

Bridged medium-sized bicyclo[m.n.2] ring systems are common in natural products and potent pharmaceuticals, and pose a great synthetic challenge. Read More

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September 2021

Concise Total Synthesis of Peyssonnoside A.

J Am Chem Soc 2021 Sep 25;143(35):14083-14088. Epub 2021 Aug 25.

Department of Chemistry, University of Zurich, Winterthurerstrasse 190, CH-8057 Zurich, Switzerland.

Peyssonnoside A is a marine-derived sulfated diterpenoid glucoside with a unique 5/6/3/6 tetracyclic skeleton with a highly substituted cyclopropane ring deeply embedded into the structure. Herein, we report the first total synthesis of this natural product in a concise, efficient, scalable, and highly diastereoselective fashion. The aglucone peyssonnosol was synthesized in 21% overall yield after 15 steps, featuring a Simmons-Smith cyclopropanation and Mukaiyama hydration, fully controlled by the spatial structure of the substrates. Read More

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September 2021

A unified strategy to prostaglandins: chemoenzymatic total synthesis of cloprostenol, bimatoprost, PGF, fluprostenol, and travoprost guided by biocatalytic retrosynthesis.

Chem Sci 2021 Aug 1;12(30):10362-10370. Epub 2021 Jul 1.

Engineering Center of Catalysis and Synthesis for Chiral Molecules, Department of Chemistry, Fudan University 220 Handan Road Shanghai 200433 P. R. China

Development of efficient and stereoselective synthesis of prostaglandins (PGs) is of utmost importance, owing to their valuable medicinal applications and unique chemical structures. We report here a unified synthesis of PGs cloprostenol, bimatoprost, PGF, fluprostenol, and travoprost from the readily available dichloro-containing bicyclic ketone guided by biocatalytic retrosynthesis, in 11-12 steps with 3.8-8. Read More

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Stereoselective Synthesis of (4,5)-5-Vinyloxazolidin-2-one-4-carboxylate as a β-Vinylserine Synthetic Equivalent by Vinyl Grignard Addition to an -Tosyl Version of Garner's Aldehyde.

Synlett 2021 10;32(6):601-604. Epub 2020 Nov 10.

Department of Chemistry, Colgate University, 13 Oak Drive, Hamilton, NY 13346, USA.

A highly efficient synthesis of a β-vinylserine synthetic equivalent is reported that exploits the stereodirecting effect of the -toluenesulfonamide in an -diastereoselective (8.5:1) vinyl Grignard addition to an analogue of Garner's aldehyde. Both aryl and alkyl Grignards are shown to give increased -selectivity compared with -Boc Garner's aldehyde. Read More

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November 2020

General Pyrrolidine Synthesis via Iridium-Catalyzed Reductive Azomethine Ylide Generation from Tertiary Amides and Lactams.

ACS Catal 2021 Jun 9;11(12):7489-7497. Epub 2021 Jun 9.

Department of Chemistry, Chemistry Research Laboratory, University of Oxford, 12 Mansfield Road, Oxford OX1 3TA, United Kingdom.

An iridium-catalyzed reductive generation of both stabilized and unstabilized azomethine ylides and their application to functionalized pyrrolidine synthesis via [3 + 2] dipolar cycloaddition reactions is described. Proceeding under mild reaction conditions from both amide and lactam precursors possessing a suitably positioned electron-withdrawing or a trimethylsilyl group, using 1 mol% Vaska's complex [IrCl(CO)(PPh)] and tetramethyldisiloxane (TMDS) as a terminal reductant, a broad range of (un)stabilized azomethine ylides were accessible. Subsequent regio- and diastereoselective, inter- and intramolecular dipolar cycloaddition reactions with variously substituted electron-deficient alkenes enabled ready and efficient access to structurally complex pyrrolidine architectures. Read More

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An Electrochemical Approach to Designer Peptide α-Amides Inspired by α-Amidating Monooxygenase Enzymes.

J Am Chem Soc 2021 Aug 21;143(30):11811-11819. Epub 2021 Jul 21.

Research School of Chemistry, Australian National University, Canberra, ACT 2601, Australia.

Designer C-terminal peptide amides are accessed in an efficient and epimerization-free approach by pairing an electrochemical oxidative decarboxylation with a tandem hydrolysis/reduction pathway. Resembling Nature's dual enzymatic approach to bioactive primary α-amides, this method delivers secondary and tertiary amides bearing high-value functional motifs, including isotope labels and handles for bioconjugation. The protocol leverages the inherent reactivity of C-terminal carboxylates, is compatible with the vast majority of proteinogenic functional groups, and proceeds in the absence of epimerization, thus addressing major limitations associated with conventional coupling-based approaches. Read More

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Total Synthesis of the Chlorinated Pentacyclic Indole Alkaloid (+)-Ambiguine G.

J Am Chem Soc 2021 Jul 19;143(29):10872-10875. Epub 2021 Jul 19.

Department of Chemistry, University of Chicago, 5735 South Ellis Avenue, Chicago, Illinois 60637, United States.

Reported herein is the total synthesis of (+)-ambiguine G, the first member of the chlorinated pentacyclic ambiguines to yield to chemical synthesis. The synthesis is accomplished through a convergent strategy that proceeds in 10 steps from ()-carvone oxide. Pivotal to the concise route is the successful realization of a [4+3] cycloaddition that conjoins two easily synthesized components of the carbon framework of the natural product. Read More

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Tandem Catalytic Indolization/Enantioconvergent Substitution of Alcohols by Borrowing Hydrogen to Access Tricyclic Indoles.

Angew Chem Int Ed Engl 2021 09 13;60(38):20689-20694. Epub 2021 Aug 13.

Department of Chemistry, National University of Singapore, 3 Science Drive 3, Singapore, 117543, Singapore.

An efficient tandem catalysis method is achieved for the direct conversion of alcohol-containing alkynyl anilines to valuable chiral 2,3-fused tricyclic indoles. This method relies on a tandem indolization followed by enantioconvergent substitution of alcohols via borrowing hydrogen to construct two rings in one step, enabled by relay and cooperative catalysis of a chiral iridium complex with a chiral phosphoric acid. Highly diastereoselective transformations of the tricyclic indole products also provide efficient access to a diverse array of complex polycyclic indoline compounds. Read More

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September 2021

Diastereoselective sp C-O Bond Formation via Visible Light-Induced, Copper-Catalyzed Cross-Couplings of Glycosyl Bromides with Aliphatic Alcohols.

ACS Catal 2020 Jun 29;10(11):5990-6001. Epub 2020 Apr 29.

Department of Chemistry, Wayne State University, Detroit, Michigan 48202, United States.

Copper-catalyzed cross-coupling reactions have become one of the most powerful methods for generating carbon-heteroatom bonds, an important framework of many organic molecules. However, copper-catalyzed C(sp)-O cross-coupling of alkyl halides with alkyl alcohols remains elusive because of the sluggish nature of oxidative addition to copper. To address this challenge, we have developed a catalytic copper system, which overcomes the copper oxidative addition barrier with the aid of visible light and effectively facilitates the cross-couplings of glycosyl bromides with aliphatic alcohols to afford C(sp)-O bonds with high levels of diastereoselectivity. Read More

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Catalytic Diastereo- and Enantioconvergent Synthesis of Vicinal Diamines from Diols through Borrowing Hydrogen.

Angew Chem Int Ed Engl 2021 08 16;60(34):18599-18604. Epub 2021 Jul 16.

Department of Chemistry, National University of Singapore, 3 Science Drive 3, Singapore, 117543, Republic of Singapore.

We present herein an unprecedented diastereoconvergent synthesis of vicinal diamines from diols through an economical, redox-neutral process. Under cooperative ruthenium and Lewis acid catalysis, readily available anilines and 1,2-diols (as a mixture of diastereomers) couple to forge two C-N bonds in an efficient and diastereoselective fashion. By identifying an effective chiral iridium/phosphoric acid co-catalyzed procedure, the first enantioconvergent double amination of racemic 1,2-diols has also been achieved, resulting in a practical access to highly valuable enantioenriched vicinal diamines. Read More

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Total Synthesis of (+)-Erogorgiaene and the Pseudopterosin A-F Aglycone via Enantioselective Cobalt-Catalyzed Hydrovinylation.

Chemistry 2021 Aug 26;27(45):11574-11579. Epub 2021 Jun 26.

University of Cologne, Greinstrasse 4, 50939, Koeln, Germany.

Due to their pronounced bioactivity and limited availability from natural resources, metabolites of the soft coral Pseudopterogorgia elisabethae, such as erogorgiaene and the pseudopterosines, represent important target molecules for chemical synthesis. We have now developed a particularly short and efficient route towards these marine diterpenes exploiting an operationally convenient enantioselective cobalt-catalyzed hydrovinylation as the chirogenic step. Other noteworthy C-C bond forming transformations include diastereoselective Lewis acid-mediated cyclizations, a Suzuki coupling and a carbonyl ene reaction. Read More

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Synthesis of Rhodium Complexes with Chiral Diene Ligands via Diastereoselective Coordination and Their Application in the Asymmetric Insertion of Diazo Compounds into E-H Bonds.

Angew Chem Int Ed Engl 2021 Aug 13;60(34):18712-18720. Epub 2021 Jul 13.

A.N. Nesmeyanov Institute of Organoelement Compounds, Russian Academy of Sciences, 28 Vavilova str., Moscow, Russia.

A new method for the synthesis of chiral diene rhodium catalysts is introduced. The readily available racemic tetrafluorobenzobarrelene complexes [(R -TFB)RhCl] were separated into two enantiomers via selective coordination of one of them with the auxiliary S-salicyl-oxazoline ligand. One of the resulting chiral complexes with an exceptionally bulky diene ligand [(R,R-iPr -TFB)RhCl] was an efficient catalyst for the asymmetric insertion of diazoesters into B-H and Si-H bonds giving the functionalized organoboranes and silanes with high yields (79-97 %) and enantiomeric purity (87-98 % ee). Read More

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Coupling of Styrylmalonates with Furan and Benzofuran Carbaldehydes: Synthesis and Chemistry of Substituted (4-Oxocyclopent-2-enyl)malonates.

J Org Chem 2021 06 28;86(12):8489-8499. Epub 2021 May 28.

N. D. Zelinsky Institute of Organic Chemistry, Russian Academy of Sciences, 47 Leninsky prosp., 119991 Moscow, Russian Federation.

On the basis of the reaction of β-styrylmalonates with furfural derivatives in the presence of GaCl that occurs with opening of the furan ring, an efficient diastereoselective method for the synthesis of trisubstituted cyclopentenones containing a 1,4-diketone moiety was developed. The regularities of the reaction were studied, and a number of chemical reactions of the resulting substrates were carried out. A mechanism for the formation of substituted (4-oxo-2-arylcyclopent-2-enyl)malonates was suggested. Read More

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Stereodivergent Strategy in Structural Determination: Asymmetric Total Synthesis of Garcinol, Cambogin, and Related Analogues.

Org Lett 2021 Jun 24;23(11):4203-4208. Epub 2021 May 24.

School of Pharmacy, Shanghai University of Traditional Chinese Medicine, Shanghai 201203, China.

The asymmetric total synthesis of five biologically significant polycyclic polyprenylated acylphloroglucinols (PPAPs), including garcinol and cambogin, was achieved through a highly diastereoselective and stereodivergent strategy. Along the way, an efficient cascade Dieckmann cyclization was employed to construct the bicyclo[3.3. Read More

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Design, synthesis and application of spiro[4.5]cyclohexadienones one-pot sequential -hydroxybenzylation/oxidative dearomatization.

Chem Commun (Camb) 2021 Jun;57(45):5574-5577

Department of Organic Synthesis and Process Chemistry, CSIR-Indian Institute of Chemical Technology (CSIR-IICT), Hyderabad 500007, India. and Academy of Scientific and Innovative Research (AcSIR), Ghaziabad 201002, India.

One-pot sequential p-hydroxybenzylation/oxidative dearomatization/spiroannulation has been designed for the efficient construction of tetrahydrofuran containing spiro-cyclohexadienones. This reaction proceeds through the p-hydroxybenzylation of 1,3-diketones with p-hydroxybenzyl alcohol via quinone methide formation followed by oxidative dearomatization/spiroannulation with suitable alcohols. The Friedel-Crafts alkylation of spiro[4. Read More

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Copper-catalyzed [3 + 2]-cycloaddition of α-halonitroalkenes with azomethine ylides: facile synthesis of multisubstituted pyrrolidines and pyrroles.

Org Biomol Chem 2021 Apr;19(15):3413-3427

N. D. Zelinsky Institute of Organic Chemistry, Russian Academy of Sciences, Leninsky prosp. 47, Moscow, 119991, Russia.

An efficient route for the synthesis of multifunctionalized pyrrolidines based on copper-catalyzed diastereoselective [3 + 2]-cycloaddition of nitroalkenes with azomethine ylides was developed. Novel fluorinated heterocycles - β-fluoro-β-nitropyrrolidines - were accessed via this method. The products can be prepared in good to excellent yields and with high diastereoselectivity. Read More

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Regio- and diastereoselective synthesis of trans-3,4-diaryldihydrocoumarins via metal-free [4+2] annulation of ynamides with o-hydroxybenzyl alcohols.

Chem Commun (Camb) 2021 May 21;57(41):5032-5035. Epub 2021 Apr 21.

Institute of New Materials & Industry Technology, College of Chemistry & Materials Engineering, Wenzhou University, Wenzhou 325035, China.

An efficient regio- and diastereoselective method for the construction of valuable trans-3,4-diaryldihydrocoumarins via metal-free [4+2] annulation of ynamides with o-hydroxybenzyl alcohols has been developed. Ynamides are first treated as 2-π partners to react with o-hydroxybenzyl alcohols via traceless sulfonamide directing groups, affording trans-3,4-diaryldihydrocoumarins in good yields with high regio- and diastereoselectivities. This metal-free methodology is also characterized by a wide substrate scope, good functional group tolerance, and efficiency on a gram scale. Read More

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Regio- and Diastereoselective Copper-Catalyzed Carbomagnesiation for the Synthesis of Penta- and Hexa-Substituted Cyclopropanes.

Angew Chem Int Ed Engl 2021 05 14;60(21):11804-11808. Epub 2021 Apr 14.

Schulich Faculty of Chemistry, Technion-Israel Institute of Technology, Technion City, Haifa, 3200009, Israel.

Despite the highly strained nature of cyclopropanes possessing three vicinal quaternary carbon stereocenters, the regio- and diastereoselective copper-catalyzed carbomagnesiation reaction of cyclopropenes provides an easy and efficient access to these novel persubstituted cyclopropyl cores with a complete regio- and diastereoselectivity. Read More

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Rhodium-Catalyzed C-H Alkenylation/Electrocyclization Cascade Provides Dihydropyridines That Serve as Versatile Intermediates to Diverse Nitrogen Heterocycles.

Acc Chem Res 2021 04 19;54(7):1766-1778. Epub 2021 Mar 19.

Department of Chemistry, Yale University, New Haven, Connecticut 06520, United States.

Nitrogen heterocycles are present in approximately 60% of drugs, with nonplanar heterocycles incorporating stereogenic centers being of considerable interest to the fields of medicinal chemistry, chemical biology, and synthetic methods development. Over the past several years, our laboratory has developed synthetic strategies to access highly functionalized nitrogen heterocycles with multiple stereogenic centers. This approach centers on the efficient preparation of diverse 1,2-dihydropyridines by a Rh-catalyzed C-H bond alkenylation/electrocyclization cascade from readily available α,β-unsaturated imines and alkynes. Read More

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Tuning Orbital Symmetry of Iridium Nitrenoid Enables Catalytic Diastereo- and Enantioselective Alkene Difunctionalizations.

J Am Chem Soc 2021 03 5;143(10):3993-4004. Epub 2021 Mar 5.

Department of Chemistry, Korea Advanced Institute of Science and Technology (KAIST), Daejeon 34141, Korea.

Among the central themes in synthetic chemistry is the establishment of novel strategies that usher in the development of more efficient and mild reactions and also expand the chemical space for asymmetric catalysis. Herein, we present an approach to revitalize the Cp*Ir(κ-LX) system as a catalyst toward alkene difunctionalizations via a nitrenoid-mediated pathway. A key strategy is tuning the orbital symmetry of the key Ir nitrenoid intermediates by ligand modification to impart the desired catalytic activity with the suppression of catalyst deactivation. Read More

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New Methods and Strategies in the Synthesis of Terpenoid Natural Products.

Acc Chem Res 2021 03 17;54(6):1347-1359. Epub 2021 Feb 17.

Department of Chemistry, University of California, Irvine, California 92697-2025, United States.

Indoloterpenoids of the paxilline type belong to a large family of secondary metabolites that exhibit unique molecular architectures and a diverse set of biological activities. More than 100 congeners identified to date share a common structural motif that contains an indole moiety fused to a rearranged diterpenoid fragment. The representative physiological and cellular effects attributed to this family of natural products include neurological and insecticidal activities, modulation of lipid balance, and inhibition of mitosis. Read More

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Enantioselective Synthesis of Cyclic Nitrones by Chemoselective Intramolecular Allylic Alkylation of Oximes.

Angew Chem Int Ed Engl 2021 04 18;60(18):9913-9918. Epub 2021 Mar 18.

Laboratorium für Organische Chemie, HCI H335, Eidgenössische Technische Hochschule Zürich, Vladimir-Prelog-Weg 3, 8093, Zürich, Switzerland.

The enantio- and chemoselective iridium-catalyzed N-allylation of oximes is described for the first time. Intramolecular kinetic resolution provides access to cyclic nitrones and enantioenriched aliphatic allylic alcohols. Salient features of this transformation are its ability to employ E/Z-isomeric mixtures of oxime starting materials convergently and high functional group tolerance. Read More

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Tetracyclic Diterpenoid Synthesis Facilitated by ODI-Cascade Approaches to Bicyclo[3.2.1]octane Skeletons.

Acc Chem Res 2021 02 28;54(4):875-889. Epub 2021 Jan 28.

Advanced Research Institute and Department of Chemistry, Taizhou University, Taizhou 318000, China.

Tetracyclic diterpenoids (C) mainly refer to the plant terpenoids bearing biogenetically related carbon skeletons derived from copalyl diphosphates (-CPP and -CPP). This large family contains over 1600 known members that can be categorized into 11 major structural types. Among them, more than three-quarters share a bridged bicyclo[3. Read More

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February 2021

Development and application of a high throughput assay system for the detection of Rieske dioxygenase activity.

Org Biomol Chem 2021 01 13;19(4):775-784. Epub 2021 Jan 13.

Department of Chemistry, Ball State University, 2000 W Riverside Ave, Muncie, IN 47306, USA.

Herein we report the development of a new periodate-based reactive assay system for the fluorescent detection of the cis-diol metabolites produced by Rieske dioxygenases. This sensitive and diastereoselective assay system successfully evaluates the substrate scope of Rieske dioxygenases and determines the relative activity of a rationally designed Rieske dioxygenase variant library. The high throughput capacity of the assay system enables rapid and efficient substrate scope investigations and screening of large dioxygenase variant libraries. Read More

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January 2021

Facile access to [1,2]-oxazine derivatives via annulations of aminoxy-tethered 1,7-enynes.

Org Biomol Chem 2021 01 6;19(4):809-821. Epub 2021 Jan 6.

Department of Organic Synthesis & Process Chemistry, CSIR-Indian Institute of Chemical Technology, Hyderabad - 500007, India. and Academy of Scientific and Innovative Research (AcSIR), Ghaziabad 201 002, India.

An efficient approach for the highly diastereoselective construction of functionalized cyclopenta[d][1,2]oxazines via sequential oxyamination and Pauson-Khand reaction of readily accessible propargylic alcohols has been developed. Furthermore, the ring closing metathesis of these N-O linked 1,7-enynes afforded vinylated-[1,2]oxazines in good yields. The reduction of the N-O bond of the obtained cyclopenta[d][1,2]oxazine is accomplished to access cyclopentenone-based amino alcohols. Read More

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January 2021

An efficient diastereoselective synthesis of novel fused 5H-furo[2,3-d]thiazolo[3,2-a]pyrimidin-5-ones via one-pot three-component reaction.

Mol Divers 2021 Jan 3. Epub 2021 Jan 3.

Department of Chemistry, Tulane University, New Orleans, LA, USA.

Herein, a convenient and efficient synthesis of 7-benzoyl-6-(aryl)-6,7-dihydro-5H-furo[2,3-d]thiazolo[3,2-a]pyrimidin-5-one derivatives was achieved from the reaction of isoquinolinium N-ylides, aromatic aldehydes, and heterocyclic 1,3-dicarbonyl compounds via one-pot three-component diastereoselective domino reaction in good-to-excellent yields. The advantages of this protocol are easily available starting materials, operational simplicity, and avoidance of hazardous organic solvents and catalyst. The synthesized products were characterized by IR, H NMR, C NMR and mass spectra. Read More

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January 2021

Intramolecular Sakurai Allylation of Geminal Bis(silyl) Enamide with Indolenine. A Diastereoselective Cyclization To Form Functionalized Hexahydropyrido[3,4-]Indole.

Org Lett 2021 01 21;23(1):124-128. Epub 2020 Dec 21.

Key Laboratory of Drug-Targeting and Drug Delivery System of the Education Ministry and Sichuan Province, Sichuan Engineering Laboratory for Plant-Sourced Drug and Sichuan Research Center for Drug Precision Industrial Technology, West China School of Pharmacy, Sichuan University, Chengdu, 610041, China.

A fluoride-promoted intramolecular Sakurai allylation of geminal bis(silyl) enamide with indolenine has been developed. The reaction facilitates an efficient cyclization to give hexahydropyrido[3,4-]indoles in good yields with high diastereoselectivity. The resulted , -stereochemistry further enables the ring-closing metathesis (RCM) reaction of two alkene moieties, giving a tetracyclic -hetereocycle widely found as the core structure in akuammiline alkaloids. Read More

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January 2021