合成医薬品の研究(第2報) Pyrrolo[1,2-d][1,4]benzodiazepine誘導体の合成

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概要

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• Conversion of 10b-phenyl-1,10b-dihydropyrrolo[2,1-α]isoquinoline-3,6(2H 5H)-diones (IIIa-c) to pyrrolo-benzodiazepine derivatives was investigated. The Beckmann rearrangement of the oximes of IIIa-c with polyphosphoric acid gave 10b-phenyl-1,10b-dihydropyrrolo[2,1-a]isoquinoline-3,5,6(2H)-triones (VIIa-c) as major products and IIIa-c, instead of the expected normal rearrangement products (VIIIa-c or XIVa-c). The Schmidt reaction of IIIa, b afforded two isomers of the rearrangement products; 11b-phenyl-7,11b-dihydro-1H-pyrrolo[1,2-d] [1,4] benzodiazepine-3,6(2H, 5H)-diones (VIIIa, b) and 11b-phenyl-5,11b-dihydro-1H-pyrrolo[2,1-d][2,4]benzodiazepine-3,7(2H, 6H)-diones (XIVa, b), together with VIIa, b. Similar treatment of IIIc, however, resulted in formation of a sole product VIIc. A number of derivatives of VIIIa, b were synthesized for pharmacological evaluation.

• 社団法人日本薬学会の論文
• 1977-02-25

著者

• 斉藤 清一

  Research Laboratories, Tanabe Seiyaku Co., Ltd.

• 斉藤 清一

  Organic Chemistry Research Laboratory Tanabe Seiyaku Co . Ltd.

• 山脇 泰彦

  田辺製薬株式会社有機化学研究所

• 渡辺 正夫

  田辺製薬株式会社有機化学研究所

• 山村 志郎

  田辺製薬株式会社有機化学研究所

• 斎藤 清一

  田辺製薬株式会社有機化学研究所

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