申请人:Mitsubishi Chemical Corporation
公开号:US20020042523A1
公开(公告)日:2002-04-11
A process for producing 1H-3-aminopyrrolidine and derivatives thereof is disclosed. The process is especially useful for producing optically active 1H-3-aminopyrrolidine and derivatives thereof and in this case comprises reacting an optically active amino-protected aspartic anhydride represented by the formula (1) with a primary amine represented by the formula R′NH
2
, subjecting the reaction product to cyclodehydration to obtain an optically active 1 -aralkyl-3-(protected amino)pyrrolidine-2,5-dione compound represented by the formula (2), subsequently eliminating the protective group from the 3-position amino group of the compound represented by the formula (2) to obtain an optically active 1-aralkyl-3-aminopyrrolidine-2,5-dione compound represented by the formula (3), reducing the carbonyl groups of the compound represented by the formula (3) to obtain either an optically active 1-aralkyl-3-aminopyrrolidine compound represented by the formula (4) or a salt thereof with a protonic acid, and then subjecting the compound represented by the formula (4) or the salt thereof to hydrogenolysis to obtain an optically active 1H-3-aminopyrrolidine or a protonic acid salt thereof.
公开了一种生产1H-3-氨基吡咯烷及其衍生物的方法。该方法特别适用于生产光学活性的1H-3-氨基吡咯烷及其衍生物,其中包括将公式(1)表示的光学活性氨基保护的天冬氨酸酐与公式R'NH2表示的一级胺反应,将反应产物经过环化脱水作用得到公式(2)表示的光学活性1-芳基甲基-3-(保护氨基)吡咯烷-2,5-二酮化合物,随后消除公式(2)所表示的化合物中3位氨基基团的保护基,得到公式(3)表示的光学活性1-芳基甲基-3-氨基吡咯烷-2,5-二酮化合物,将公式(3)所表示的化合物的羰基基团还原,得到公式(4)表示的光学活性1-芳基甲基-3-氨基吡咯烷化合物或其与质子酸的盐,然后将公式(4)所表示的化合物或其盐进行氢解,得到光学活性的1H-3-氨基吡咯烷或其质子酸盐。