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Chinese Chemical Letters 2024年第2期35卷 366-369页

作者： Qiao Li Minjie Liu Meifen Jiang Li Wan Yingtang Ning fen-er chen College of Chemical Engineering Zhejiang University of TechnologyHangzhou 310014China Engineering Center of Catalysis and Synthesis for Chiral Molecules Fudan UniversityShanghai 200433China Shanghai Engineering Center of Industrial Catalysis for Chiral Drugs Shanghai 200433China Institute of Pharmaceutical Science and Technology Zhejiang University of TechnologyHangzhou 310014China

We report the photo-mediated 1,2-aryl migration of 2‑chloro-1-arylpropanones to 2-arylpropionic acids using HCOONa as an acid *** pragmatically focused study obviates the multiple-step sequence in the industrially employed,ZnO-promoted rearrangement strategy,and offers rapid access to various 2-arylpropionic acids under environmentally friendly ***,the successful transfer of this batch photochemistry to a continuous flow platform led to improved scalability and enabled the gram-scale synthesis of loxoprofen.

关键词： Green chemistry Flow chemistry 2-Arylpropionic acids Photo-Favorskii reaction

Palladium-catalyzed stereoselective decarboxylative[4+2]cyclization of 2-methylidenetrimethylene carbonates with pyrrolidone-derived enones:Straightforward access to chiral tetrahydropyran-fused spiro-pyrrolidine-2,3-diones

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Chinese Chemical Letters 2024年第6期35卷 279-282页

作者： Ke Zhang Sheng Zuo Pengyuan You Tong Ru fen-er chen Key Laboratory of Natural Medicines of the Changbai Mountain Ministry of EducationCollege of PharmacyYanbian UniversityYanji 133002China College of Chemistry and Chemical Engineering Jiangxi Normal UniversityNanchang 330022China Engineering Center of Catalysis and Synthesis for Chiral Molecules Fudan UniversityShanghai 200433China Shanghai Engineering Center of Industrial Catalysis for Chiral Drugs Shanghai 200433China

A novel asymmetric[4+2]cycloaddition of 2-methylidenetrimethylene carbonate with pyrrolidonederived enones has been achieved to produce the functionalized tetrahydropyran-fused spirocyclic scaffolds via *** array of enantioenriched spiro-pyrrolidine-2,3-diones bearing adjacent quaternary and tertiary stereocenters are obtained in high yields with excellent enantioselectivities(up to 96% yield and 99% ee).The further transformation of the product has been accomplished for the construction of medical interesting β^(2,2)-amino acids and β-*** mechanistic research was well conducted.

关键词： Pyrrolidine-2,3-diones 2-Methylidenetrimethylene carbonate Asymmetric annulation Spiroheterocycles Allylic 1,3-strain

Nitrite-catalyzed economic and sustainable bromocyclization of tryptamines/tryptophols to access hexahydropyrrolo[2,3-b]indoles/tetrahydrofuroindolines in batch and flow

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Chinese Chemical Letters 2024年第7期35卷 247-252页

作者： Xiao Xiao Biao chen Jia-Wei Li Jun-Bo Zheng Xu Wang Hang Zhao fen-er chen Institute of Pharmaceutical Science and Technology Collaborative Innovation Center of Yangtze River Delta Region Green PharmaceuticalsZhejiang University of TechnologyHangzhou 310014China College of Chemistry and Chemical Engineering Jiangxi Normal UniversityNanchang 330022China Engineering Center of Catalysis and Synthesis for Chiral Molecules Department of ChemistryFudan UniversityShanghai 200433China Shanghai Engineering Center of Industrial Asymmetric Catalysis for Chiral Drugs Shanghai 200433China

A highly efficient and concise bromocyclization has been successfully achieved,in which tryptamine/tryptophol derivates can be transformed to valuable HPI/TFI scaffolds with economic and green ***,a controllable cascade transformation of bromocyclization and aromatic bromination has also been smoothly achieved to form dibrominated HPIs and *** could be successfully scaled up under both the batch process and a continuous flow *** most remarkable peculiarity of our process over all previous methods is that the generated water is the major ***,successful application of this new protocol has been demonstrated by the pharmaceutical and natural products syntheses.

关键词： Tryptamines and tryptophols Nitrite Economic and sustainable bromocyclization HPI and TFI structures Bath and flow

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八步连续流全合成维生素B_(1)工艺研究

Engineering 2024年第1期32卷 226-232页

作者： Meifen Jiang Minjie Liu Weijian Li Yingqi Xia fen-er chen Engineering Center of Catalysis and Synthesis for Chiral Molecules Department of ChemistryFudan UniversityShanghai 200433China Shanghai Engineering Research Center of Industrial Asymmetric Catalysis of Chiral Drugs Shanghai 200433China School of Science Harbin Institute of Technology(Shenzhen)Shenzhen 518055China

Vitamin B_(1) is widely applied in the healthcare and food industry as an antineuritic and antioxidant to maintain the normal functioning of nerve conduction,the heart,and the gastrointestinal *** study reports on an integrated eight-step continuous-flow synthesis of vitamin B_(1) from commercially available *** proposed continuous-flow process is based on advances in chemistry,engineering,and equipment design,and affords improved performance and safety compared with batch-mode *** challenges were precisely investigated and controlled,including mixing,unexpected clogging,solvent switches,an exothermic reaction,and the prevention of side reactions,using various micro-channel flow reactors,mixers,separators,and continuous *** B_(1) was produced with a separated yield of 47.7% and high purity,with a total residence time of about 3.5 *** eight-step continuous-flow protocol enables technology involving up to six of the key principles of green ***,the application of flow technology is of paramount importance for improving security,reducing waste,and,in particular,improving the efficiency of batch operations that require several days for manufacturing.

关键词： Vitamin B_(1) Continuous-flow synthesis Micro-reactor Continuous manufacturing

Asymmetric catalytic anhydride openings via carbon-based nucleophiles

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Chinese Chemical Letters 2014年第1期25卷 1-8页

作者： chen Zheng fen-er chen Department of Chemistry Fudan University

The asymmetric desymmetrization of cyclic anhydrides via the addition of carbon-based nucleophiles has been the focus of considerable levels of interest because it leads to optically active products. Over the past 20 years, a variety of different catalytic asymmetric alkylation reactions have been developed for the desymmetrization of cyclic anhydrides using different metal reagents as nucleophiles and using chiral ligands. The purpose of this review is to provide an overview of significant developments in this field. ~ 2013 fen-er chen. Published by Elsevier B.V. on behalf of Chinese Chemical Society. All rights reserved.

关键词： Cyclic anhydrides Carbon-based nucleophiles Chiral ligands Asymmetric catalysis Metal reagents

A family of novel bifunctional organocatalysts:Highly enantioselective alcoholysis of meso cyclic anhydrides and its application for synthesis of the key intermediate of P2X_7 receptor antagonists

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Chinese Chemical Letters 2013年第7期24卷 553-558页

作者： Hong-Jun Yang Fang-Jun Xiong Jie Li fen-er chen Department of Chemistry Fudan University Institute of Biomedical Science Fudan University

A family of novel squaramides/sulfamides based on 1,2-alkamine was developed as chiral bifunctional catalysts to promote the asymmetric alcoholysis of meso cyclic anhydrides. The hemiesters were obtained in high yield with up to 93% ee. The usefulness of this methodology was demonstrated in the asymmetric synthesis of the key intermediate of P2X7 receptor antagonists.

关键词： Asymmetric alcoholysis Bifunctional organocatalyst Cyclic anhydrides P2X7 receptor antagonists Sulfamides

Studies on a New Usage of Hypophosphorous Acid-iodine System in N-C Bond Cleavage

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Chinese Chemical Letters 2003年第4期14卷 351-354页

作者： Ge MENG Ling ZHAO You Fu LUO fen er chen Department of Chemistry Fudan UniversityShanghai 200433

A mixture of hypophosphorous acid (H3PO2) and iodine in acetic acid can cleave the N-alkyl bond in a variety of N-1 substituted pyrimidine derivative in relatively high yields, without any damage to the amido bond in ... 详细信息

关键词： Hypophosphorous acid iodine carbon-nitrogen bond cleavage.

Synthesis of rac-α-aryl propionaldehydes via branched-selective hydroformylation of terminal arylalkenes using water-soluble Rh-PNP catalyst

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Chinese Chemical Letters 2022年第2期33卷 830-834页

作者： Peng Gao Miaolin Ke Tong Ru Guanfeng Liang fen-er chen Department of Chemistry Sichuan UniversityChengdu 610064China Department of Chemistry Fudan UniversityShanghai 200433China Shanghai Engineering Center of Industrial Asymmetric Catalysis for Chiral Drugs Fudan UniversityShanghai 200433China

This work detailed the preparation of a class of water-soluble PNP ligands that differed by the nature of the substitute on phenyl ring of ligands. These ligands were incorporated into water-soluble rhodium-PNP complex catalysts that were used to regioselective hydroformylation of a series of terminal arylalkenes,providing efficient access to rac-α-aryl propionaldehydes in good to excellent yield(up to 97%) and branched-regioselectivity(up to 40:1 b/l ratio). Furthermore, gram-scale and diverse synthetic transformation demonstrated synthetic application of this methodology for non-steroidal antiinflammatory drugs.

关键词： Aryl propionaldehydes Hydroformylation Water-soluble PNP ligands Regioselectivity Rhodium

Picomolar inhibitor of reverse transcriptase featuring significantly improved metabolic stability

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药学学报:英文版 2023年第7期13卷 3054-3066页

作者： Ya-Li Sang Christophe Pannecouque erik De Clercq Shuai Wang fen-er chen Department of Chemistry Engineering Center of Catalysis and Synthesis for Chiral MoleculesFudan UniversityShanghai 200433China Shanghai Engineering Center of Industrial Asymmetric Catalysis for Chiral Drugs Shanghai 200433China School of Science Harbin Institute of Technology(Shenzhen)Shenzhen 518055China Rega Institute for Medical Research KU LeuvenLeuven B-3000Belgium

Considering the undesirable metabolic stability of our recently identified NNRTI 5(t1/2=96 min)in human liver microsomes,we directed our efforts to improve its metabolic stability by introducing a new favorable hydroxymethyl side chain to the C-5 position of *** strategy provided a series of novel methylol-biphenyl-diarylpyrimidines with excellent anti-HIV-1 *** best compound 9g was endowed with remarkably improved metabolic stability in human liver microsomes(t1/2=2754 min),which was about 29-fold longer than that of 5(t1/2=96 min).This compound conferred picomolar inhibition of WT HIV-1(EC50=0.9 nmol/L)and low nanomolar activity against five clinically drug-resistant mutant *** maintained particularly low cytotoxicity(CC50=264μmol/L)and good selectivity(SI=256,438).Molecular docking studies revealed that compound 9g exhibited a more stable conformation than 5 due to the newly constructed hydrogen bond of the hydroxymethyl group with ***,compound 9g was characterized by good safety *** displayed no apparent inhibition of CYP enzymes and h *** acute toxicity assay did not cause death and pathological damage in mice at a single dose of 2 g/*** findings paved the way for the discovery and development of new-generation anti-HIV-1 drugs.

关键词： NNRTI HIV-1 DAPYs Picomolar Metabolic stability

Chemical and chemoenzymatic stereoselectivesynthesis of β-nucleosides and their analogues

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Organic Chemistry Frontiers 2022年第6期9卷 1719-1741页

作者： Hui-Jing Wang Yang-Yang Zhong You-Cai Xiao fen-er chen Sichuan Research Center for Drug Precision Industrial Technology West China School of PharmacySichuan UniversityChengdu610041China Engineering Center of Catalysis and Synthesis for Chiral Molecules Department of ChemistryFudan UniversityShanghai200433China Shanghai Engineering Center of Industrial Asymmetric Catalysis for Chiral Drugs Shanghai 200433ChinaShanghai200433China

β-Nucleosides are fundamental building blocks of biological systems and are widely used as therapeuticagents for the treatment of cancer and viral infections, among others. In the last two years, nucleosideanalogues have been investigated with renewed urgency in the search for agents that are effective againstSARS-CoV-2, the cause of the ongoing global pandemic of COVID-19. This has resulted in an explosionof activities in the field of β-nucleoside synthesis. This review summarizes the historical perspective andthe recent advances in the stereoselective synthesis of β-nucleosides and their analogues. The syntheticstrategies to obtain β-nucleosides can be divided into three categories: (1) N-glycosylation;(2) intramolecular sugar ring formation;and (3) enzymatic transglycosylation.

关键词： synthesis analogues nucleoside