申请人:Celgene Corporation
公开号:US05424454A1
公开(公告)日:1995-06-13
L-alanyl-L-proline is stereoselectively prepared catalytically hydrogenating an N-(2-iminopropionyl)-L-proline in the presence of a metal hydrogenolysis catalyst and at a pH of less than about 4. Also disclosed are improved processes for production of N-pyruvyl-L-proline in which L-proline and a 2,2-disubstituted propionyl halide are allowed to react at a pH of at least 9 to produce an L-proline intermediate which is hydrolyzed at a pH range of from about 6.5 to about 8.5 to yield N-pyruvyl-L-proline.
L-丙氨酰-L-脯氨酸可在金属氢解催化剂存在下,以及在pH小于约4的条件下,对N-(2-亚胺基丙酰基)-L-脯氨酸进行立体选择性制备催化氢化。还披露了改进的生产N-丙酰基-L-脯氨酸的过程,其中L-脯氨酸和2,2-二取代丙酰卤在pH至少为9的条件下反应,产生L-脯氨酸中间体,在pH范围从约6.5到约8.5的条件下水解,得到N-丙酰基-L-脯氨酸。