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【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