β-内酰胺酶抑制剂他唑巴坦的合成

摘要本文对 3α -甲基 - 7-氧代 - 3β - ( 1H - 1 ,2 ,3-三唑 - 1 -甲基 ) - 4-硫杂 - 1-氮杂双环 [3,2 ,0 ]庚烷 - 2α -羧酸 - 4,4 -二氧化物 (他唑巴坦 )的合成进行了研究 ,尤其对其中的氯化环合和叠氮化两步反应的影响因素进行了系统研究。试验以6 -APA为原料 ,经重氮化溴化、氧化、氯化环合等 1 1步反应 ,最终得到了 4 %收率的他唑巴坦

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	曹琳
	陈立功
	李阳
	白国义
	王铮

关键词：他唑巴坦 β-内酰胺酶抑制剂 6-APA 氯化环合

Abstract： The synthesis of 3α-methyl-7-oxo-3β-(1H-1,2,3 triazol-1-ylmethyl)-4-thia-azobicyelo[3,2,0] heptane 2α-carboxylic acid-4,4-dioxide(tazobactam) was studied in this paper, particularly the affecting factors of the chlorization cyclization and azide substitution. The synthesis of tazobactam was described starting with 6-aminopenicillanic acid in eleven steps, that include diazotization-bromination, oxidation, chlorization cyclization and so on. Finally tazobactam was obtained and the total yield was about 4%.

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Received 2002-05-15; published 2002-05-15

引用本文:

曹琳,陈立功,李阳,白国义,王铮.β-内酰胺酶抑制剂他唑巴坦的合成[J]. 化学工业与工程, 2002,19(3): 219-224

CAO Lin, CHEN Li-gong, LI Yang, BAI Guo-yi, WANG Zheng .Synthesis of the β-Lactamase Inhibitor Tazobactam[J]. Chemcial Industry and Engineering, 2002,19(3): 219-224