1-(tert-butyl)-4-phenyl-1,2,3,6-tetrahydropyridine -Drug Synthesis Database

【结构式】

【分子编号】24876

【品名】1-(tert-butyl)-4-phenyl-1,2,3,6-tetrahydropyridine

【CA登记号】

【分子式】C₁₅H₂₁N

【分子量】215.33848

【元素组成】C 83.67% H 9.83% N 6.5%

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：(III)

There are several synthetic pathways leading to title compound which are depicted in Scheme. Generally, 1-alkyl-4,4 diphenylpiperidines Iike budipine are accessible in a simple manner and with attractive yields by a regioselective reaction of piperidine derivatives such as (I), (II), (III) or, par ticularly, 3-aroyl-4-aryl-4-hydroxypiperidines (IV) with benzene under Friedel Crafts' conditions.

参考文献中间体

合成目标

【1】 Schaefer, H.; Eistetter, K.; Klosa, J.; Menge, H.G.; Hackmack, G.; 4,4-Diphenylpiperidines - A new class of potent central stimulants. 5th Intl Symp Med Chem (July 19-22, Paris) 1976, Abst 052.
【2】 Hackmack, S.H.; et al.; Synthesis physical-chemical properties and pharmacologically-oriented screening studies on budipine and related 4,4-diphenylpiperidines. Arzneim-Forsch Drug Res 1984, 34, 3, 233.
【3】 Shaefer, H.; et al. (Byk Gulden Lomberg Chemische Fabrik GmbH); Alkylsubstituierte piperidin-N-oxide, verfahren zu ihrer herstellung. Ihre verwendung und sie enthaltende Arzneimittel. DE 2825322 .
【4】 Koch, H.; Budipine. Drugs Fut 1985, 10, 8, 621.

中间体序号	中间体编号	品名	分子式	供应商	用于合成
(I)	24874	methyl 1-(tert-butyl)-4-phenyl-4-piperidinecarboxylate	C₁₇H₂₅NO₂	详情	详情
(II)	24875	1-(tert-butyl)-4-piperidinone; N-(tert-butyl)-4-piperidinone	C₉H₁₇NO	详情	详情
(III)	24876	1-(tert-butyl)-4-phenyl-1,2,3,6-tetrahydropyridine	C₁₅H₂₁N	详情	详情
(IV)	24877	[1-(tert-butyl)-4-hydroxy-4-phenyl-3-piperidinyl](phenyl)methanone	C₂₂H₂₇NO₂	详情	详情

Extended Information