(2S,4R)-1-叔丁氧羰基-4-甲烷磺酰氧基吡咯烷-2-羧酸的合成研究

Synthesis of (2S, 4R)-1-(tert-butoxycarbonyl)-4-((methylsulfonyl)oxy)pyrrolidine-2-carboxylic Acid

以反式-4-羟基-L-脯氨酸为原料,先经Boc保护,再与甲烷磺酰氯反应,2步合成了药物中间体(2S,4R)-1-叔丁氧羰基-4-甲烷磺酰氧基吡咯烷-2-羧酸,总收率为80.4%。考察了温度、溶剂等反应条件对收率的影响,产物结构经MS,1H-NMR确证。

The drug intermediate（2S,4R）-1-（tert-butoxycarbonyl）-4-（（methylsulfonyl）oxy）pyrrolidine-2-carboxylic acid was obtained from trans-4-Hydroxy-Lproline wia 2-step reactions,the total yield was 80.4 %.The effect of reaction conditions on the yield of reaction was investigated.The target compound was indentified by MS and1H-NMR.