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微生物酶催化碳氢键的不对称氧化反应合成手性4-氯二苯基甲醇*
http://www.100md.com 2014年9月10日 遵义医科大学学报 2014年第1期
药学院,1Introduction,2Experiments,3Resultsanddiscussions,4Conclusion
     陈永正,杨 敏,卓俊睿,郑代军,付少彬

    (遵义医学院药学院,贵州遵义 563099)

    1 Introduction

    Chiral sec-alcohols were key intermediate in the synthesis of fine chemicals,pharmaceuticals,and agrochemicals[1].Chiral benzhydrol was one kind of important building block for synthesis of orphenadrine 1,neobenodine 2,carbinoxamine 3[2].Moreover,chiral benzhydrol was also used as an intermediate of some potent anti-inflammatory drugs 4 and ODE-Ⅳ inhibitor.

    Currently,numerous syntheses of chiral benzhydrol mainly depended on reduction of ketones,hydrolysis of esters and kenetic resolution of racemic alcohols with chemical catalyst or biocatalyst[3].For example,a new γ - amino thiol was designed for synthesis of chiral benzhydrol by asymmetric arylation of aromatic aldehydes[4].The addition reaction of organoboronic acids with aldehydes catalyzed by CoI2/(R,R)-BDPP also give chiral benzhydrol in excellent yields with 90% ~ 99%ee[5-6].Truppo group reported that a reductase catalyzed the reduction of di- aryl ketones to produce chiral benzhydrol[7]. ......

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