A process for production of cyclopropyl-fused pyrrolidine-based inhibitors of dipeptidyl peptidase IV is provided which employs a BOC-protected amine of the structure
prepared by subjecting an acid of the structure
to reduce amination by treating the acid with ammonium formate, nicotinamide adenine dinucleotide, dithiothreitol and partially purified phenylalanine dehydrogenase/formate dehydrogenase enzyme concentrate (PDH/FDH) and without isolating treating the resulting amine of the structure 2
with di-tert-butyl dicarbonate to form the BOC-protected amine
提供了一种生产环丙基融合
吡咯烷基
二肽酶IV
抑制剂的方法,该方法采用结构为的BOC保护胺,其制备方法为:通过将结构为的酸与
甲酸铵、烟酰胺
腺嘌呤二核苷酸、二
硫苏糖醇和部分纯化的苯丙氨酸脱氢酶/
甲酸脱氢酶酶浓缩物(PDH/FDH)进行还原胺化处理,而无需分离处理得到结构为2的胺,然后使用二叔丁基二
碳酸酯对其进行保护。