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Synthesis of 7- (2-dimethylaminovinyl) derivatives of pyrazolo[1,5-a] pyrimidines, as precursors of new tricyclic series. Binding studies of BDZ receptor

Bruni, F.; Costanzo, A.; Selleri, S.; Guerrini, G.; Giusti, L.; Martini, C.; Lucacchini, A.

Farmaco 48(2): 309-319

1993

ISSN/ISBN: 0014-827X
PMID: 8388217
Document Number: 410469
A series of 7-dimethylaminovinylpyrazolo[1,5-a]pyrimidines bearing an acetyl or an ethoxycarbonyl group at the 6-position turned out to be useful intermediates for the synthesis of pyrazolo[1,5-a]pyrido[3,4-e]pyrimidines and 8H-pyrazolo[5',1':2,3]pyrimido[5,4-d][1,2]diazepines. These tricyclic derivatives were studied for their affinity for the central benzodiazepine receptor, and meaningful suggestions about the structure-affinity relationship were obtained. Some of the above intermediates were also reacted with S-methylthiourea, to give a mixture of pyrazolo[5',1':1,2]pyrimido[5,6-e][1,3]diazocines and pyrazolo[1,5-a]quinazolines.

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