An improved process for the preparation of [1S-(1R*,2S*,3R*)]-N (4-morpholinylsulfonyl)-L-phenylalanyl-3-(2-amino-4 thiazolyl)-N-[(1-cyclohexylmethyl) -2,3-dihydroxy-5-methylhexyl]-L-alaninamide is described where the key intermediate, 3-(2-amino 4-thiazolyl)-L-alanine is converted without protecting the aminothiazole group to the desired compound, as well as valuable intermediates used in the process.
本文描述了一种改进的制备[1S-(1R*,2S*,3R*)]-N(4-吗啉磺酰基)-L-苯丙
氨酰基-3-(2-
氨基-4-
噻唑基)-N-[(1-环己甲基)-2,3-二羟基-5-甲基己基]-L-丙
氨酰胺的过程,其中关键中间体3-(2-
氨基4-
噻唑基)-
L-丙氨酸在不保护
氨基
噻唑基的情况下转化为所需化合物,以及在该过程中使用的有价值的中间体。