发明申请
US20120053350A1 PREPARATION OF ALKYL ESTERS OF N-PROTECTED OXO-AZACYCLOALKYLCARBOXYLIC ACIDS
审中-公开
N-保护的氧亚氨基甲酰氧基酸的烷基酯的制备
- 专利标题： PREPARATION OF ALKYL ESTERS OF N-PROTECTED OXO-AZACYCLOALKYLCARBOXYLIC ACIDS
- 专利标题（中）： N-保护的氧亚氨基甲酰氧基酸的烷基酯的制备
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申请号： US13266871申请日： 2010-04-26
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公开(公告)号： US20120053350A1公开(公告)日： 2012-03-01
- 发明人: Ian Mangion , Mark A. Huffman , Rebecca T. Ruck , Joseph Lynch , John Y.L. Chung , Benjamin Marcune
- 申请人： Ian Mangion , Mark A. Huffman , Rebecca T. Ruck , Joseph Lynch , John Y.L. Chung , Benjamin Marcune
- 国际申请： PCT/US10/32380 WO 20100426
- 主分类号： C07D471/08
- IPC分类号： C07D471/08 ; C07D401/12 ; C07D211/60
摘要：
A process for the preparation of alkyl esters of N-protected oxo-azacycloalkylcarboxylic acids of Formula III: comprises contacting a ketosulfoxonium ylide of Formula II: with an iridium catalyst to obtain Compound III, wherein PG1 is an amine protective group; k is 0, 1, or 2; and RU, R1, R2, and R3 are defined herein. An embodiment of the process further com rises contacting a compound of Formula I: with a sulfoxonium halide of formula (RU)3S(O)Z, wherein Z is halide, in the presence of a strong base to obtain Compound II. Additional embodiments add a series of process steps leading to the synthesis of 7-oxo-1,6-diazabicyclo[3.2.1]octanes suitable for use as β-lactamase inhibitors.
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