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【结 构 式】

【分子编号】33766

【品名】4-amino-1-butanol

【CA登记号】13325-10-5

【 分 子 式 】C4H11NO

【 分 子 量 】89.13748

【元素组成】C 53.9% H 12.44% N 15.71% O 17.95%

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:(VII)

Coupling of 4-aminobutanol (VII) with 4-phenylbenzoyl chloride (VIII) produced hydroxy amide (IX). Further Swern oxidation of the alcohol group of (IX) using oxalyl chloride and DMSO afforded aldehyde (X). Finally, reductive condensation of aldehyde (X) with pyrrolidine (VI) in the presence of NaBH(OAc)3 afforded the title compound.

1 Audinot, V.; Dubuffet, T.; Newman-Tancredi, A.; Cussac, D.; Millan, M.J.; Lavielle, G.; Loutz, A.; Novel benzopyrano[3,4-c]pyrrole derivatives as potent and selective dopamine D3 receptor antagonists. Bioorg Med Chem Lett 1999, 9, 14, 2059.
2 Lejeune, F.; Hautefaye, P.; Millan, M.; Dubuffet, T.; Lavielle, G. (ADIR et Cie.); Chromene derivs., process for their preparation and pharmaceutical compsns. containing them. EP 0887350; JP 1999071376; US 6090837 .
中间体序号 中间体编号 品名 CAS号 分子式 供应商 用于合成
(VI) 33765 (3aR,9bS)-1,2,3,3a,4,9b-hexahydrochromeno[3,4-c]pyrrole-8-carbonitrile C12H12N2O 详情 详情
(VII) 33766 4-amino-1-butanol 13325-10-5 C4H11NO 详情 详情
(VIII) 28439 [1,1'-biphenyl]-4-carbonyl chloride 14002-51-8 C13H9ClO 详情 详情
(IX) 33767 N-(4-hydroxybutyl)[1,1'-biphenyl]-4-carboxamide C17H19NO2 详情 详情
(X) 33768 N-(4-oxobutyl)[1,1'-biphenyl]-4-carboxamide C17H17NO2 详情 详情
Extended Information