79100-16-6Relevant articles and documents
MODULAR SYNTHESES OF DISCOIPYRROLE TYPE ALKALOIDS AND ANALOGUES
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, (2017/07/06)
The present invention relates to methods for preparing a variety of discoipyrrole compounds and analogues using an oxidative cyclisation reaction as one of the steps. The present invention also relates to novel discoipyrrole analogues, pharmaceutical comp
New method of synthesis of 5,6-dihydro-4H-pyrrolo[1,2-a]-[1,4] benzodiazepines
Mokrov, Grigory V.,Likhosherstov, Arkady M.,Gewald, Rainer,Schindler, Rudolf
experimental part, p. 2713 - 2722 (2011/04/17)
2,5-Dimethoxy-2-(dimethoxymethyl)tetrahydrofuran 1 reacted with anthranilic acid alkyl esters 2 in boiling acetic acid to give 2-(2-formylpyrrol-1-yl) benzoic acid esters 3. The reductive amination of 3 with primary arylalkylamines 4 led to 2-{2-[(arylalkylamino)methyl]pyrrol-1-yl}-benzoic acids esters 5. Heating of the aminoesters 5 in xylene under reflux resulted in 5-(arylalkyl)-4,5-dihydro-6H-pyrrolo[1,2-a][1,4]benzodiazepin-6-ones 7. Lactams 7 were reduced by lithium aluminum hydride in toluene and and ether solutions to give 5-(arylalkyl)-5,6-dihydro-4H-pyrrolo[1,2-a][1,4]benzodiazepines 8. The solid products 8 were recrystallized and the liquid ones were transformed into their salts with oxalic acid. The Japan Institute of Heterocyclic Chemistry.