申请人:——
公开号:US20040236118A1
公开(公告)日:2004-11-25
The object of the invention is to provide a process for efficient, inexpensive and stereoselective production of (2S,4S)-2-[[(3R)-pyrrolidin-3-yl-(R)-hydroxylmethyl]pyrrolidin-4-thiol dihydrochloride useful as an intermediate in production of novel carbapenem, and the intermediate is produced via a novel crystallizable intermediate (2S,4R)—N-t-butoxycarbonyl-2-[[(3R)—N-t-butoxycarbonyl pyrrolidin-3-yl-(R)-hydroxylmethyl]-4-hydroxypyrrolidine from a (2S,4R)-4-alkylsilyloxy-N-t-butoxycarbonylpyridine-2-carbaldehyde derivative by aldol reaction using an asymmetric assistant such as amino-alcohol.
本发明的目的是提供一种高效、廉价和立体选择性生产(2S,4S)-2-[[(3R)-吡咯啉-3-基-(R)-羟甲基]吡咯啉-4-硫醇二盐酸盐的方法,该方法是通过使用一种新的可结晶中间体(2S,4R)-N-叔丁氧羰基-2-[[(3R)-N-叔丁氧羰基吡咯啉-3-基-(R)-羟甲基]-4-羟基吡咯烷通过使用氨基醇等不对称助剂的醛缩反应从(2S,4R)-4-烷基硅氧基-N-叔丁氧羰基吡啶-2-甲醛衍生物中制备的,该中间体可用作新型头孢菌素的中间体。