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[3-二烷基氨基取代的2H-1,4-苯并恶嗪]

[3-Dialkylamino-substituted 2H-1,4-benzoxazines].

作者信息

Balbi A, Ferreccio R, Mazzei M, Ermili A, Roma G

出版信息

Farmaco Sci. 1986 Dec;41(12):942-53.

PMID:3556568
Abstract

N,N,N',N'-Tetrasubstituted 2-(2-aminophenoxy)malonamides (IX) in the presence of phosphorus oxychloride led to the formation of N,N-dialkyl-3-(dialkylamino)-2H-1,4-benzoxazine-2-carboxamides (XII). In the same way 2-(2-amino-3-pyridyloxy)-N,N,N',N'-tetraethylmalonamide (X) yielded 3-(diethylamino)-N,N-diethyl-2H-pyrido[3,2-b] [1,4]oxazine-2-carboxamide (XIII). Also N,N-dialkyl-2-(2-aminophenoxy)acetamides (XIV) by the action of phosphorus oxychloride afforded 3-(dialkylamino)-2H-1,4-benzoxazines (XV). Some compounds when submitted to pharmacological screening showed a weak depressant activity in the Irwin test.

摘要

在三氯氧磷存在下,N,N,N',N'-四取代的2-(2-氨基苯氧基)丙二酰胺(IX)生成了N,N-二烷基-3-(二烷基氨基)-2H-1,4-苯并恶嗪-2-甲酰胺(XII)。同样,2-(2-氨基-3-吡啶氧基)-N,N,N',N'-四乙基丙二酰胺(X)生成了3-(二乙氨基)-N,N-二乙基-2H-吡啶并[3,2-b][1,4]恶嗪-2-甲酰胺(XIII)。此外,N,N-二烷基-2-(2-氨基苯氧基)乙酰胺(XIV)在三氯氧磷作用下生成了3-(二烷基氨基)-2H-1,4-苯并恶嗪(XV)。一些化合物在进行药理筛选时,在欧文试验中显示出微弱的抑制活性。

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