【结 构 式】 |
【分子编号】28465 【品名】(2S,3S)-3-amino-1-[1-[4-(2-methyl-2H-1,2,3,4-tetraazol-5-yl)benzyl]hydrazino]-4-phenyl-2-butanol 【CA登记号】 |
【 分 子 式 】C19H25N7O 【 分 子 量 】367.45408 【元素组成】C 62.11% H 6.86% N 26.68% O 4.35% |
与该中间体有关的原料药合成路线共 1 条
合成路线1
该中间体在本合成路线中的序号:(XX)In a variation of this procedure, aryl tetrazole (II) was alkylated with ICH3 to provide methyltetrazole (XV). Condensation of (XV) with tert-butyl carbazate afforded hydrazone (XVI), which was reduced to the benzylhydrazine (XVII) by means of NaBH3CN and p-toluenesulfonic acid. Opening of the Boc-protected epoxide (XVIII) with hydrazine (XVII) gave hydrazinoalcohol (XIX). Acid deprotection of both Boc groups of (XIX) furnished diamino compound (XX), which was finally coupled with N-methoxycarbonyl-L-tert-leucine (X) by means of TPTU.
【1】 New aza-dipeptide analogues as potent and orally a. J Med Chem 1998, 41, 18, 3387. |
【2】 Fassler, A.; Bold, G.; Capraro, H.-G.; Lang, M.; Khanna, S.C. (Novartis AG); Antivirally active heterocyclic azahexane derivs.. EP 0900210; JP 1999511177; US 5849911; WO 9740029 . |
中间体序号 | 中间体编号 | 品名 | CAS号 | 分子式 | 供应商 | 用于合成 |
---|---|---|---|---|---|---|
(II) | 28449 | 4-(2H-1,2,3,4-tetraazol-5-yl)benzaldehyde | 74815-22-8 | C8H6N4O | 详情 | 详情 |
(X) | 23447 | (2S)-2-[(methoxycarbonyl)amino]-3,3-dimethylbutyric acid | C8H15NO4 | 详情 | 详情 | |
(XV) | 28461 | 4-(2-methyl-2H-1,2,3,4-tetraazol-5-yl)benzaldehyde | C9H8N4O | 详情 | 详情 | |
(XVI) | 28462 | tert-butyl 2-[(Z)-[4-(2-methyl-2H-1,2,3,4-tetraazol-5-yl)phenyl]methylidene]-1-hydrazinecarboxylate | C14H18N6O2 | 详情 | 详情 | |
(XVII) | 28463 | tert-butyl 2-[4-(2-methyl-2H-1,2,3,4-tetraazol-5-yl)benzyl]-1-hydrazinecarboxylate | C14H20N6O2 | 详情 | 详情 | |
(XVIII) | 23444 | tert-butyl (1S)-1-[(2R)oxiranyl]-2-phenylethylcarbamate | C15H21NO3 | 详情 | 详情 | |
(XIX) | 28464 | tert-butyl 2-[(2S,3S)-3-[(tert-butoxycarbonyl)amino]-2-hydroxy-4-phenylbutyl]-2-[4-(2-methyl-2H-1,2,3,4-tetraazol-5-yl)benzyl]-1-hydrazinecarboxylate | C29H41N7O5 | 详情 | 详情 | |
(XX) | 28465 | (2S,3S)-3-amino-1-[1-[4-(2-methyl-2H-1,2,3,4-tetraazol-5-yl)benzyl]hydrazino]-4-phenyl-2-butanol | C19H25N7O | 详情 | 详情 |
Extended Information