【结 构 式】 |
【药物名称】 【化学名称】1-[N-(Benzyloxycarbonyl)-L-leucyl-glycyl]pyrrolidine-2(S)-carbonitrile 【CA登记号】 【 分 子 式 】C21H28N4O4 【 分 子 量 】400.48171 |
【开发单位】CNRS (Originator), Universidade de Brasilia (Originator) 【药理作用】ANTIINFECTIVE THERAPY, Antitrypanosomals, Treatment of Protozoal Diseases |
合成路线1
Prolinamide (I) was coupled with Z-leucylglycine (II) in the presence of DCC and HOBt to give the tripeptide amide (III). The terminal carboxamido group of (III) was then dehydrated to the corresponding nitrile by treatment with SOCl2 and N-methylmorpholine.
【1】 Santana, J.; Gullet, C.; Schrével, J.; Frappier, F.; Maoulida, C.; Grellier, P.; Joyeau, R.; Teixeira, A.R.L.; Synthesis and activity of pyrrolidinyl- and thiazolidinyl-dipeptide derivatives as inhibitors of the Tc80 prolyl oligopeptidase from Trypanosoma cruzi. Eur J Med Chem 2000, 35, 2, 257. |
中间体序号 | 中间体编号 | 品名 | CAS号 | 分子式 | 供应商 | 用于合成 |
---|---|---|---|---|---|---|
(I) | 36137 | (2S)-2-pyrrolidinecarboxamide;L-prolinamide | 7531-52-4 | C5H10N2O | 详情 | 详情 |
(II) | 46318 | 2-[((2S)-2-[[(benzyloxy)carbonyl]amino]-4-methylpentanoyl)amino]acetic acid | C16H22N2O5 | 详情 | 详情 | |
(III) | 46319 | benzyl (1S)-1-[([2-[(2S)-2-(aminocarbonyl)pyrrolidinyl]-2-oxoethyl]amino)carbonyl]-3-methylbutylcarbamate | C21H30N4O5 | 详情 | 详情 |
Extended Information