An efficient chemoenzymatic route to the antidepressants (R)-fluoxetine and (R)-tomoxetine

被引:22
作者
Bracher, F [1 ]
Litz, T [1 ]
机构
[1] TECH UNIV CAROLO WILHELMINA BRAUNSCHWEIG,INST PHARMAZEUT CHEM,D-38106 BRAUNSCHWEIG,GERMANY
关键词
D O I
10.1016/0968-0896(96)00077-6
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
(S)-1-Phenyl-3-buten-1-ol (1), prepared in high optical purity by enzymatic resolution of the racemate, is a convenient building block for the synthesis of (R)-fluoxetine (7a) and (R)-tomoxetine (7b). Compound 1 was converted to the title drugs by etherification with appropriate phenols under Mitsunobu conditions, ozonolysis of the terminal double bond, mesylation of the resulting alcohol and substitution with methylamine. Copyright (C) 1996 Elsevier Science Ltd
引用
收藏
页码:877 / 880
页数:4
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