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化学学报
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化学学报 ›› 1982, Vol. 40 ›› Issue (5): 458-462. 上一篇    下一篇

研究简报

全合成先锋霉素的重要中间体—噻嗪酸酯的研究

王序1, 王泽民2, 练汝丰2   

  1. 1. 北京医学院;
    2. 北京制药工业研究所
  • 投稿日期:1980-06-19 发布日期:2013-06-03
  • 通讯作者: 练汝丰

STUDY ON ALKYL 6H-1, 3-THIAZINE-4-CARBOXYLATE——AN IMPORTANT INTERMEDIATE IN TOTAL SYNTHESIS OF CEPHALOSPORIN

WANG XU1, WANG ZE-MIN2, LIAN RU-FENG2   

  1. 1. Beijing Medical College;
    2. Beijing Institute of Pharmaceutical Industries
  • Received:1980-06-19 Published:2013-06-03

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近年来对于先锋霉素全合成的研究有了很大的发展.已报道的全合成路线中,以Merck-Syntex[1]路线比较实用.为了合成先锋霉素的重要中间体——噻嗪酸酯3,Merck-Syntex使用了Wittig反应,步骤比较长.他们所以采用Wittig反应,是考虑到酯基旁边的α-H不够活泼,不能与甲基酮起缩合反应.

This investigation describes a new simple method for the synthesis of alkyl 6H-1, 3-thinzine-4-carboxylate, an important intermediate in the total synthesis of eephaloaporin. The α-methylenP group in the intermediate, CH3COCH2SCH-NCH2CO2R, is ac6ivated both by the adjacent N=CH structure and the ester csarbonyl group.