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[摘要]：anthranilic acid alkyl esters in boiling acetic acid to give 2-(2-formylpyrrol-1-yl)benzoic acid esters. The reductive amination of these esters with primary arylalkylamines led to 2-{2-[(arylalkylamino)methyl]pyrrol-1-yl}benzoic acids esters, e.g., I. Heating of the aminoesters in xylene under reflux resulted in 5-(arylalkyl)-4,5-dihydro-6H-pyrrolo[1,2-a][1,4]benzodiazepin-6-ones, e.g., II. These lactams were reduced by lithium aluminum hydride in toluene and ether solns. to give 5-(arylalkyl)-5,6-dihydro-4H-pyrrolo[1,2-a][1,4]benzodiazepines. The solid products were recrystd. and the liq. ones were transformed into their salts with oxalic acid. |
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