[N-α-（对甲苯磺酰甘氨酰脯氨酰）-4-脒基苯丙氨酸酰胺作为凝血酶抑制剂的合成]

[Synthesis of N-alpha-(tosylglycylprolyl)-4-amidinophenylalanine amides as thrombin inhibitors].

作者信息

Voigt B, Wagner G

出版信息

Pharmazie. 1986 Jun;41(6):378-81.

Abstract

N alpha-(Tosylprolylglycyl)-4-cyanphenylalanine was synthesized by the reaction of an activated ester and a mixed anhydride, respectively, of Tos-Pro-Gly-OH with 4-cyanophenylalanine. N alpha-(Tosylglycylprolyl)-4-cyanophenylalanine was prepared by reaction of Tos-Gly-Cl with N alpha-prolyl-4-cyanophenylalanine. These acids were transferred into the amides. The cyano compounds were converted into the desired amidines via the thioamides and the thioimidic esters.

摘要

通过使对甲苯磺酰基 - 脯氨酰 - 甘氨酸（Tos - Pro - Gly - OH）的活化酯和混合酸酐分别与4 - 氰基苯丙氨酸反应，合成了Nα - （对甲苯磺酰基脯氨酰基甘氨酰基） - 4 - 氰基苯丙氨酸。通过对甲苯磺酰基甘氨酸氯（Tos - Gly - Cl）与Nα - 脯氨酰基 - 4 - 氰基苯丙氨酸反应制备了Nα - （对甲苯磺酰基甘氨酰基脯氨酰基） - 4 - 氰基苯丙氨酸。这些酸被转化为酰胺。氰基化合物通过硫代酰胺和硫代亚胺酯转化为所需的脒。

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