AN EFFICIENT SYNTHESIS OF A KEY INTERMEDIATE TOWARDS (S)-(-)-NADIFLOXACIN

被引:17
作者
MORITA, S
OTSUBO, K
MATSUBARA, J
OHTANI, T
UCHIDA, M
机构
[1] Tokushima Research Institute, Otsuka Pharmaceutical Co., Ltd., Tokushima, 771-01, Kagasuno 463-10, Kawauchi-cho
关键词
D O I
10.1016/0957-4166(94)00381-K
中图分类号
O61 [无机化学];
学科分类号
070301 ; 081704 ;
摘要
An efficient and highly enantioselective synthesis of (S)-(-)-5,6-difluoro-2-methyl-1,2,3,4-tet (4b), a key intermediate in the synthesis of (S)-(-)-nadifloxacin (2), was carried out by using a cross-coupling reaction. Also alpha,beta-acetylenic ketones 14a,b underwent an asymmetric reduction using various chiral reagents to afford the corresponding propargylic alcohols 8a,b in good yield and excellent enantiomeric excess, which can be easily converted to butanol 9.
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页码:245 / 254
页数:10
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