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asymmetric synthesis of N-(Diphenylphosphinyl)furfurylamine by the Enantioselective Alkylation of Furfurylimine

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Chinese Chemical Letters 2005年第9期16卷 1147-1150页

作者： Hai Le ZHANG Xiao Mei ZHANG Xin LI Ai Qiao MI Xin CUI Yao Zhong JIANG Key laboratory of asymmetric synthesis and Chirotechnology of Sichuan Province and union Laboraotry of asymmetric synthesis Chengdu Institute of Organic Chemistry Chinese Academy of Sciences Chengdu 610041

Optically active N-（diphenylphosphinyl）furfurylamines 2 with good ee values were obtained by the enantioselective addition of dialkylzincs to furfuryl imine 1 in the presence of chiral aminoalcohol derivatives and o... 详细信息

关键词： asymmetric dialkylzinc N-(diphenylphosphinyl)furfurylarnine.

Copper-Catalyzed Enantioselective synthesis of α-Hydroxyamine Using Monodentate Phosphoramidites

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有机化学 2004年第Z1期24卷 43-44页

作者： DONG,Lin CUN,Lin-Feng GONG,Liu-Zhu MI,Ai-Qiao JIANG,Yao-Zhong Key laboratory of asymmetric synthesis and Chirotechnology of Sichuan Province and union laboratory of asymmetric synthesis Chengdu Institute of Organic Chemistry Chinese Academy of Sciences Chengdu 610041 Key Laboratory of Asymmetric Synthesis and Chirotechnology of Sichuan Province and Union Laboratory of Asymmetric Synthesis Chengdu Institute of Organic Chemistry Chinese Academy of Sciences Chengdu 610041 Key Laboratory of Asymmetric Synthesis and Chirotechnology of Sichuan Province and Union Laboratory of Asymmetric Synthesis Chengdu Institute of Organic Chemistry Chinese Academy of Sciences Chengdu 610041 Key Laboratory of Asymmetric Synthesis and Chirotechnology of Sichuan Province and Union Laboratory of Asymmetric Synthesis Chengdu Institute of Organic Chemistry Chinese Academy of Sciences Chengdu 610041 Key Laboratory of Asymmetric Synthesis and Chirotechnology of Sichuan Province and Union Laboratory of Asymmetric Synthesis Chengdu Institute of Organic Chemistry Chinese Academy of Sciences Chengdu 610041

　　Development of new methods for the introduction of a nitrogen atom to a carbonyl group is still the most important synthetic target. Cu-catalyzed addition of organozinc reagents to α,β-unsaturated carbonyl compounds has been the subject of intensive investigation.[1] Moreover, trapping of the intermediate Zn-enolates has been achieved using nitrosobenzene. To demonstrate the feasibility of developing enantioselective variants of these tandem C-C bond formations,α,β-unsaturated substrates a～d was subjected to standard reaction conditions using Feringa's (L1*, L2*) and our own phosphoramidite ligands (L3*, L4*). In this reaction, medium to high levels of enantioselectivities were observed.……

关键词： carbonyl compounds methods for

Tunable Dendritic Ligands of Chiral 1,2-Diamine and Their Application in asymmetric Transfer Hydrogenation

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有机化学 2004年第Z1期24卷 49-50页

作者： LIU,Wei-Guo CUI,Xin CUN,Lin-Feng WU,Jun ZHU,Jin DENG,Jin-Gen Key laboratory of asymmetric synthesis & Chirotechnology of Sichuan Province and union laboratory of asymmetric synthesis Chengdu Institute of Organic Chemistry Chinese Academy of Sciences Chengdu 610041 Key Laboratory of Asymmetric Synthesis & Chirotechnology of Sichuan Province and Union Laboratory of Asymmetric Synthesis Chengdu Institute of Organic Chemistry Chinese Academy of Sciences Chengdu 610041 Key Laboratory of Asymmetric Synthesis & Chirotechnology of Sichuan Province and Union Laboratory of Asymmetric Synthesis Chengdu Institute of Organic Chemistry Chinese Academy of Sciences Chengdu 610041 Key Laboratory of Asymmetric Synthesis & Chirotechnology of Sichuan Province and Union Laboratory of Asymmetric Synthesis Chengdu Institute of Organic Chemistry Chinese Academy of Sciences Chengdu 610041 Key Laboratory of Asymmetric Synthesis & Chirotechnology of Sichuan Province and Union Laboratory of Asymmetric Synthesis Chengdu Institute of Organic Chemistry Chinese Academy of Sciences Chengdu 610041 Key Laboratory of Asymmetric Synthesis & Chirotechnology of Sichuan Province and Union Laboratory of Asymmetric Synthesis Chengdu Institute of Organic Chemistry Chinese Academy of Sciences Chengdu 610041

　　Dendrimers are perfect monodisperse macromolecules with a regular and highly branched three-dimensional architecture, so their unique physical and chemical properties are noticed and utilized more and more.[1] The dendrimer architecture can offer a means of better controlling the disposition of the catalytic species in soluble polymer-based catalysts and such novel catalysts of nano-scale size may aid the recycling of catalysts simply by supra-filtration or solvent precipitation methods.……

关键词： precipitation methods chemical properties

synthesis and preliminary cytotoxic evaluation of substituted indoles as potential anticancer agents

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Chinese Chemical Letters 2007年第8期18卷 899-901页

作者： Chang Qing Shi Zhang Qin Liu Wen Qing Lin Yuan Wei Chen Key laboratory of asymmetric synthesis ＆ Chirotechnology of Sichuan Province and union laboratory of asymmetric synthesis Chengdu Institute of Organic Chemistry Chinese Academy of Sciences Chengdu 610041 China Graduate School of Chinese Academy of Sciences Beijing 100049 China

A variety of indole derivatives were designed, synthesized and preliminarily evaluated for their in vitro cytotoxic activity in the A431 and H460 cell lines. All the compounds examined conferred unusual potency in a tumor cell cytotoxicity assay. The findings showed the indole derivatives would be a promising candidate for the development of new anticancer agents.

关键词： Indoles synthesis Kinesin spindle protein inhibitor Cytotoxicity Cancer treatment

synthesis of urea acetates as potential PPARα/γ dual agonists

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Chinese Chemical Letters 2008年第2期19卷 166-168页

作者： Chang Yan Zhao Chang Qing Shi Yuan Wei Chen Key laboratory of asymmetric synthesis ＆ Chirotechnology of Sichuan Province and union laboratory of asymmetric synthesis Chengdu Institute of Organic Chemistry Chinese Academy of Sciences Chengdu 610041 China Graduate School of Chinese Academy of Sciences Beijing 100049 China

In the quest for novel PPARα/γ dual agonists as putative drugs for the treatment of type 2 diabetes and dyslipidemia, we designed and synthesized a series of urea acetates as potential PPARα/γ dual agonists. The s... 详细信息

关键词： Oxazolc PPAR agonist Type 2 diabetes Urea Ammonolysis synthesis

Small Peptides Catalyzed Direct Aldol Reactions of Aldehydes with Hydroxyacetone with Regiocontrol in Aqueous Media

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有机化学 2004年第Z1期24卷 41-42页

作者： TANG,Zhuo YANG,Zhi-Hua CUN,Lin-Feng GONG,Liu-Zhu MI,Ai-Qiao JIANG,Yao-Zhong Key laboratory of asymmetric synthesis and Chirotechnology of Sichuan Province and union laboratory of asymmetric synthesis Chengdu Institute of Organic Chemistry Chinese Academy of Sciences Chengdu 610041

Very recently, we[1] found that L-proline amides and dipeptides acted as efficient catalysts for the asymmetric direct aldol reaction. We report here that L-proline-based peptides 1~5 can catalyze the aldol reactions of hydroxyacetone with aldehydes 6 in aqueous media, to give 1,4-diols (7), the disfavored products with either aldolase or L-proline. Both peptides 3 and 4 give good results.……

关键词： aldol reaction aqueous media

Using Natural Cinchona Alkaloids to Promote the Enantioselective Addition of Dialkylzinc to N-Diphenylphosphinylimines

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Chinese Journal of Chemistry 2003年第7期21卷 955-959页

作者：张海乐方春梅李昕龚流柱宓爱巧崔欣蒋耀忠 union laboratory of asymmetric synthesis Chengdu Institute of Organic Chemistry Chinese Academy of Sciences Chengdu Sichuan 610041 China

Cinchona alkaloids are utilized as chiral ligands to promote the enantioselective addition of dialkylzinc to N-diphenylphos-phinylimines affording enantiomerically enriched N-diphenyl-phosphinylamines in up to 91% ee.

关键词： cinchona alkaloids dialkylzinc N-diphenylphos-phinylimines

A Cell Solid Structure of cis-1,3-Cyclohexanedicarboxylic Acid and Its Complex Crystal with 4,4'-Dipyridine

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有机化学 2004年第Z1期24卷 51-52页

作者： GAO,Wei YU,Kai-Bei ZHU,Jin DENG,Jin-Gen Key laboratory of asymmetric synthesis & Chirotechnology of Sichuan Province and union laboratory of asymmetric synthesis Chengdu Institute of Organic Chemistry Chinese Academy of Sciences Chengdu 610041

Carboxylic acids are important in crystal engineering because they can form strong and directional O-H…O hydrogen bonds as dimmer and catmer.[1] The dicarboxylic acids (not containing other hydrogen bonding groups) generally form the extended line structure interlinked through dimmer,[2] except that oxalic acid forms both the β-oxalic acid linked by dimmer (finite synthon) and the a-oxalic acid by catmer[3] (infinite synthon). A new molecular packing structure of cis-1,3-cyclohexanedicarboxylic acid (CHDA), which is different from line structure,[4] was gotten (P1/2, Figure 1). The novel structure has dimmer and catmer hydrogen bond pairs in the crystal and the hydrogen bond length of O-H…O is 0.268 nm in catmer and 0.264 nm in dimmer. The bond angles of O=C-O vary from 123.1° to 123.8° in catmer and from 123.1° to 122.0° in dimmer comparing with the ones in line structure.……

关键词： oxalic acid hydrogen bonding crystal engineering molecular packing novel structure hydrogen bonds bond length

Enantio-divergent C–H borylation with two different ligands from a single chiral source

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Science China Chemistry 2025年第1期 226-232页

作者： Rongrong Du Senmiao Xu State Key laboratory for Oxo synthesis and Selective Oxidation Lanzhou Institute of Chemical Physics Chinese Academy of Sciences College of Material Chemistry and Chemical Engineering Key Laboratory of Organosilicon Chemistry and Material TechnologyMinistry of Education Hangzhou Normal University University of Chinese Academy of Sciences

Reported here is an iridium-catalyzed enantio-divergent C（sp3）–H borylation of α-gem-dimethyl groups of trifluoromethyl ketone-derived hydrazones to construct a series of acyclic all-carbon quaternary stereocenters with a high level of chiral induction. Two different chiral bidentate boryl ligands from a common chiral source not only can switch the enantioselectivity but also are complementary in terms of the substrate scope.

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