【药物名称】Gepirone hydrochloride, ORG-33062, MJ-13805, BMY-13805, Variza, Ariza
化学结构式(Chemical Structure):
参考文献No.58303
标题:2-[4-[(4,4-Dialkyl-2,6-piperidinedion-1-yl)butyl]-1-piperazinyl]pyrimidines
作者:Temple, D.L. Jr. (Bristol-Myers Squibb Co.)
来源:BE 0895504; CH 656383; DE 3248160; FR 2518993; GB 2114122; JP 1983118582; JP 1994293753; US 4423049
合成路线图解说明:

The quaternary salt (II), prepared from 1-(pyrimidin-2-yl)piperazine (I) and 1,4-dibromobutane (A), undergoes reaction with 3,3-dimethylglutarimide (III) in the presence of potassium carbonate in refluxing xylene to afford the free base (IV), which is isolated by acid extraction and basification of the extract. Treatment of the free base with HCl in isopropanol affords ttle compound as the monohydrochloride.

合成路线图解说明:

This compound has been obtained by two related ways: The reduction of 4-[4-(2-pyrimidinyl)piperazin-1-yl]butyronitrile (I) by means of RaNi and hydrazine in isopropanol gives 4-[4-(2-pyrimidinyl)piperazin-1-yl]butylamine (II), which is then condensed with 3,3-dimethylglutaric anhydride (III) in refluxing xylene or refluxing toluene to yield the target glutarimide derivative. Alternatively, the condensation of N-(4-bromobutyl)-3,3-dimethylglutarimide (IV) with 1-(2-pyrimidinyl)piperazine (V) by means of K2CO3 in refluxing acetonitrile also yields the target glutarimide derivative.

参考文献No.67201
标题:Gepirone Hydrochloride
作者:Eison, M.S.; Yevich, J.P.; Farney, R.F.
来源:Drugs Fut 1985,10(6),456
合成路线图解说明:

The quaternary salt (II), prepared from 1-(pyrimidin-2-yl)piperazine (I) and 1,4-dibromobutane (A), undergoes reaction with 3,3-dimethylglutarimide (III) in the presence of potassium carbonate in refluxing xylene to afford the free base (IV), which is isolated by acid extraction and basification of the extract. Treatment of the free base with HCl in isopropanol affords ttle compound as the monohydrochloride.

参考文献No.706446
标题:Buspirone analogues. 1. Structure-activity relationships in a series of N-aryl- and heteroarylpiperazine derivatives
作者:Yevich, J.P.; Temple, D.L. Jr.; New, J.S.; Taylor, D.P.; Riblet, L.A.
来源:J Med Chem 1983,26(2),194
合成路线图解说明:

This compound has been obtained by two related ways: The reduction of 4-[4-(2-pyrimidinyl)piperazin-1-yl]butyronitrile (I) by means of RaNi and hydrazine in isopropanol gives 4-[4-(2-pyrimidinyl)piperazin-1-yl]butylamine (II), which is then condensed with 3,3-dimethylglutaric anhydride (III) in refluxing xylene or refluxing toluene to yield the target glutarimide derivative. Alternatively, the condensation of N-(4-bromobutyl)-3,3-dimethylglutarimide (IV) with 1-(2-pyrimidinyl)piperazine (V) by means of K2CO3 in refluxing acetonitrile also yields the target glutarimide derivative.

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