PREPARATION OF 5-AMINO-1,2-DIHYDRO-4-(1-METHYL-4-PIPERIDINYL)PYRROL-3-ONES

被引：1

作者：

Chalyk, Bohdan A. ^{[1
]}

Tverdokhlebov, Anton V. ^{[1
]}

Iminov, Rustam T. ^{[2
]}

Tolmachev, Andrey A. ^{[1
,2
]}

机构：

[1] Enamine Ltd, UA-01103 Kiev, Ukraine

[2] Kiev Natl Taras Shevchenko Univ, UA-01033 Kiev, Ukraine

来源：

HETEROCYCLES | 2009年 / 78卷 / 08期

关键词：

Hydrogenation; Nitrile; Piperidine; Pyridine; Pyrrole; RECEPTOR ANTAGONISTS; NK1; ANTAGONISTS; POTENT; INHIBITORS; DESIGN; DERIVATIVES; PIPERIDINES; HETEROCYCLES; AGONISTS; KINASE;

D O I：

10.3987/COM-09-11701

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

Acylation of (1-methyl-4(1H)-pyridinylidene)acetonitrile with chloroacetyl chloride was found to occur at the exocyclic carbon atom leading to 4-chloro-2-(1-methyl-4(1H)-pyridinylidene)-3-oxobutanenitrile. Its reaction with primary amines furnished 4-(2-amino-4,5-dihydro-4-oxo-1H-pyrrol-3-yl)-1-methylpyridinium chlorides. Hydrogenation of these quaternary salts afforded 5-amino-1,2-dihydro-4-(1-methyl-4-piperidinyl)-3H-pyrrol-3-ones in nearly quantitative yields.

引用

页码：2021 / 2032

页数：12

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