6533b7cefe1ef96bd125796c

RESEARCH PRODUCT

Studies on the synthesis of heterocyclic compounds. III. Preparation of some pyrazolo[3,4-C] [1,5]benzodiazocin-10(11H)one derivatives

Vincenzo SprioGiuseppe DaidoneSalvatore Plescia

subject

chemistryStereochemistryPhosphorusYield (chemistry)Organic Chemistrychemistry.chemical_elementMedicinal chemistry

description

Starting from the readly available N-melhyl-N-(1-phenyl-3-R-pyrazol-5-yl)-2-nitrobenzamides (1a,b), the pyrazoles, 4-aeetyl substituted 2a,b, were prepared in high yield. Reduction of 2a gave the amino derivative 4a, which was eyclized to the desired pyrazolo[3,4-c][1,5]benzodiazo-cin-10(11H)one (5a). Compound 2b afforded 5b directly. Compound 5b was also prepared by the action of phosphorus oxychloride on N-methyl-N-(1,3-diphenylpyrazol-5-yl)-2-acetamido-benzamide (6b).

https://doi.org/10.1002/jhet.5570160521