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Budipine hydrochloride, BY-701, Parkinsan

布地平 Chemical Name: 1-tert-Butyl-4,4-diphenylpiperidine hydrochloride; 1-(1,1-Dimethylethyl)-4,4-diphenylpiperidine hydrochloride
CAS No. 63661-61-0, 57982-78-2 (free base)
项目整合开发状态: Launched-1997
项目研究机构: Altana Pharma (Originator), Lundbeck (Licensee)
合成路线: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.

合成路线:Condensation of 2-mercaptobenzothiazole (I) with isonicotinic acid hydrazide (INH) (II) in the presence of formaldehyde affords H-15 in 80% yield.
📌 参考资料/链接:
参考文献标题:Alkylsubstituierte piperidin-N-oxide,verfahren zu ihrer herstellung.Ihre verwendung und sie enthaltende Arzneimittel
文献作者:Shaefer,H.; et al.(Byk Gulden Lomberg Chemische Fabrik GmbH)
参考来源:DE 2825322

📄 详细内容


合成路线: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.

参考文献标题:Budipine
文献作者:Koch,H.
参考来源:Drugs Fut 1985,10(8),621


合成路线: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.

参考文献标题:Synthesis physical-chemical properties and pharmacologically-oriented screening studies on budipine and related 4,4-diphenylpiperidines
文献作者:Hackmack,S.H.; et al.
参考来源:Arzneim-Forsch Drug Res 1984,34(3),233


合成路线: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.
参考文献标题:4,4-Diphenylpiperidines - A new class of potent central stimulants
文献作者:Schaefer,H.; Eistetter,K.; Klosa,J.; Menge,H.G.; Hackmack,G.
参考来源:5th Intl Symp Med Chem (July 19-22,Paris) 1976,Abst 052


产品链接: CAS No. 63661-61-0››

产品链接: CAS No.57982-78-2››