YAKUGAKU ZASSHI
Online ISSN : 1347-5231
Print ISSN : 0031-6903
ISSN-L : 0031-6903
Diazepine誘導体の合成.(1).2-Chloro-11H-pyrimido[4,5-b][1,4]benzodiazepin-6(5H)-one誘導体の合成
伊奈 修一郎森田 邦彦野口 功
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1978 年 98 巻 1 号 p. 72-76

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4-(2-Methoxycarbonylanilino)-2-chloro-5-nitropyrimidine derivatives (IIIa-c) were prepared from methyl anthranilate derivatives (1a-c) and 2, 4-dichloro-5-nitropyrimidine. Aminopyrimidines (IVa-c) were prepared by the reduction of nitropyrimidines (IIIa-c) with stannous chloride in acetic acid. 2-Chloro-11H-pyrimido [4, 5-b] [1, 4] benzodiazepin-6 (5H)-one derivatives (Va-c) were synthesized by the intramolecular ring closure of aminopyrimidine derivatives. 2-Chloro-11-methylpyrimido [4, 5-b] [1, 4] benzodiazepin-6 (5H)-one (Vd) was obtained by the reductive cyclization of 4-(2-methoxycarbonyl-N-methylanilino)-2-chloro-5-nitropyrimidine (IIId) with stannous chloride in acetic acid.
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