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Absolute configuration of Buagafuran:An experimental and theoretical electronic circular dichroism study

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Chinese Chemical Letters 2013年第6期24卷 500-502页

作者： li li Chun li Yi-Kang Si da-li yin Beijing Key Laboratory of Active Substances Discovery and Druggability Evaluation Institute of Materia MedicaChinese Academy of Medical Sciences & Peking Union Medical College

Buagafuran is a novel drug candidate derived from natural *** absolute configuration has been confirmed by electronic circular dichroism combined with modern quantum-chemical calculation using time-dependent density functional *** predicted UV absorbance peak is underestimated by several nanometers compared with the experimental *** applicability of empirical rule for the C=C-C-O system in Buagafuran has also been *** results show that electronic circular dichroism could be a useful tool for the absolute configuration assignment of chiral drugs,especially for the oily or semisolid substances,whose crystal structures are impossible to obtain.

关键词： Electronic circular dichroism Chiral drugs Absolute configuration Time-dependent density functional theory

ECD spectrometric methods for detecting the enantioselective enzymatic hydrolysis of racemic 3-acetoxy-4-phenyl-β-lactam

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Chinese Chemical Letters 2012年第10期23卷 1197-1200页

作者： Xiang Zhang li li Yi Kang Si da li yin Beijing Key Laboratory of Active Substances Discovery and Druggability Evaluation Institute of Materia MedicaChinese Academy of Medical Sciences&Peking Union Medical CollegeBeijing 100050China

（-）-（3R, 4S）-3-Acetoxy-4-phenylazetidin-2-one （（-）-1） was the key intermediate for preparing optical C-13 side-chain moiety in partial synthesis of docetaxel and paclitaxel. It can be successfully prepared via enantioselective hydrolysis of racemic esters （（-4-）-1） catalyzed by bacterial lipases, but the current reaction evaluation method is tedious and inconvenient. Electronic circular dichroism （ECD） has been widely applied in the stereochemical study of chiral compounds. In this paper, a rapid ECD spectroscopic method has been proposed and established to detect the transformation directly. The absolute configurations of lipase-catalyzed hydrolysis products have also been confirmed by quantum-chemical calculation using time-dependent density functional theory （TDDFT） methodology.

关键词： ECD spectroscopy Evaluation method Absolute configuration Time-dependent density functional theory

A practical synthesis of (-)fosfomycin from its enantiomer

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Chinese Chemical Letters 2008年第11期19卷 1297-1300页

作者： Meng Zhang Zheng Yu Ji Jun li da li yin Beijing Collab Pharma Co. Ltd. Beijing 102600 China Institute of Materia Medica Peking Union Medical College Beijing 100050 China

（＋）-cis-（1S, 2R）-Epoxypropylphosphonic acid, the enantiomer of fosfomycin, which is the industrial side-product in the preparation of the antibiotic fosfomycin, was converted into （-）fosfomycin by a seven-step procedure. The esterification of the dihydroxyphosphonic intermediate was the key step. The title compound was obtained in good yield and its optical purity was up to the medicine quality standard of Chinese Pharmacopoeia.

关键词： Fosfomycin Enantiomer Phosphonate

A Convergent Route for the Synthesis of AF-5

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Chinese Chemical Letters 2003年第7期14卷 670-672页

作者： da li yin Ji Yu GUO Xiao Tian liANG Institute of Materia Medica Chinese Academy of Medical Sciences&Peking Union Medical CollegeBeijing 100050

AF-5 was synthesized through a convergent method. The key step was the Robinson annulation using a key intermediate pentyl vinyl ketone.

关键词： AF-5 synthesis Robinson annulation.

A Highly Regioselective Deacetylation of Taxanes

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Chinese Chemical Letters 2002年第6期13卷 501-504页

作者： Meng ZHANG da li yin Ji Yu GUO Xiao Tian liANG Institute of Materia Medica Chinese Academy of Medical Sciences&Peking Union Medical CollegeBeijing 100050

A highly regioselective O-deacetylation of taxanes at C-5 position was accomplished by treatment with t-BuOK and a possible mechanism was proposed.

关键词： Paclitaxel taxane deacetylation.

An efficient method for preparing the sphingosine-1-phosphate receptor agonist, KRP203-phosphate

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Chinese Chemical Letters 2013年第9期24卷 817-820页

作者： Xiao-Jian Wang Jian-Guo Qi Gang li Yu-lin Tian da-li yin State Key Laboratory of Bioactive Substances and Functions of Natural Medicines Beijing Key Laboratory of Active Substance Discovery and Drugability EvaluationInstitute of Materia Medica Peking Union Medical College and Chinese Academy of Medical Sciences

An efficient method for mono-phosphorylation of 2 （KRP203） using cbz-protection, dibenzylphosphoryl chloride and TMSI affording 2-P （KRP203-P） was developed. We applied the present method to the synthesis of KRP20... 详细信息

关键词： Mono-phosphorylation TMSI KRP203-P

A nucleophilic 1,3-rearrangement leading to 3,4-disubstituted 3,4-dihydroquinolines

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Chinese Chemical Letters 2016年第7期27卷 1036-1039页

作者： Chun-Xian He Zhi-Bo Jiang Hua-Qing Cui da-li yin State Key Laboratory of Bioactive Substances and Functions of Natural Medicines Institute of Materia Medica Peking Union Medical College and Chinese Academy of Medical Sciences Department of Medicinal Chemistry Beijing Key Laboratory of Active Substances Discovery and Drugability Evaluation Institute of Materia Medica Peking Union Medical College and Chinese Academy of Medical Sciences

A new nucleophilic 1,3-rearrangement is observed when treating 2-methoxyquinolino-3-lithium with an α-C substituted deoxybenzoin,and this rearrangement yielded an unusual 3,4-disubstituted 3,*** similar reactions were designed and executed to investigate this novel 1,3-rearrangement,and a mechanism involving a nucleophilic addition and a following 1,3-rearrangement with an unusual dearomatization on the quinoline ring is proposed.

关键词： 1,3-Rearrangement Dihydroquinoline derivatives Reaction mechanism

Synthesis and bio-evaluation of phenothiazine derivatives as new antituberculosis agents

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Chinese Chemical Letters 2015年第8期26卷 951-954页

作者： Chun-Xian He Hui Meng Xiang Zhang Hua-Qing Cui da-li yin State Key Laboratory of Bioactive Substances and Functions of Natural Medicines Institute of Materia Medica Peking Union Medical College and Chinese Academy of Medical Sciences College of Pharmacy Shandong University of Traditional Chinese Medicine Department of Medicinal Chemistry Beijing Key Laboratory of Active Substances Discovery and Drugability Evaluation Institute of Materia Medica Peking Union Medical College and Chinese Academy of Medical Sciences

Two series of phenothiazine derivatives were designed and synthesized. All compounds were tested for anti-tuberculosis activities against Mycobacterium tuberculosis H37RV. In comparison with mother compound of chlorpromazine, compound 6e shows promising anti-tuberculosis activity and much less mammalian cell cytotoxicity, compound 6e merits to be further explored as new anti-tuberculosis agents.

关键词： tuberculosis mother Mycobacterium cytotoxicity dimethylamino likely moiety mammalian alkyl phenoxy

Entry into Major Groups Retaining Taxol via Sinenxan A

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Chinese Chemical Letters 2002年第2期13卷 135-138页

作者： Meng ZHANG da li yin Ji Yu GUO Xiao Tian liANG Institute of Materia Medica Chinese Academy of Medical Science&Peking Union Medical CollegeBeijing 100050

Compound 1 as a key intermediate of 1, 7, 9-trideoxytaxol was synthesized in ten steps from a biosynthetically available taxane, Sinenxan A. The key steps in the synthesis were deoxygenation at C-14, allylic oxidatio... 详细信息

关键词： Taxol Sinenxan A deoxygenation.