Voigt B, Wagner G
Pharmazie. 1985 May;40(5):305-6.
Based on 4-cyanophenylalanine, the title compounds had been obtained by benzyloxycarbonylation of the amino group, subsequent formation of the activated ester by 4-nitrophenol, its aminolysis and at least change of the cyano function to the amidine function via thiocarbamides and thioimid acid esters. The inhibitor effect against thrombin of the pyrrolidid 16 is analogous to those of the adequate N alpha-tosyl compound.
基于4-氰基苯丙氨酸,通过氨基的苄氧羰基化、随后用4-硝基苯酚形成活性酯、其氨解以及至少通过硫脲和硫代亚氨酸酯将氰基官能团转变为脒官能团,得到了标题化合物。吡咯烷16对凝血酶的抑制作用与相应的Nα-甲苯磺酰化合物类似。