METHOD FOR PREPARING DERIVATIVES OF PYRAZOLOPYRIMIDINONE FOR TREATMENT OF IMPOTENCY Russian patent published in 2004 - IPC

Abstract RU 2236410 C2

FIELD: organic chemistry, chemical technology, medicine.

SUBSTANCE: invention relates to a method for preparing derivatives of pyrazolopyrimidinone of the formula (1):

wherein R1 represents (C1-C4)-alkyl; R2 represents substituted or unsubstituted (C2-C4)-alkyl; R3 represents substituted or unsubstituted (C2-C6)-alkyl; R4 represents substituted or unsubstituted (C1-C6)-alkyl, substituted or unsubstituted (C3-C6)-alkyl, substituted or unsubstituted phenyl, substituted or unsubstituted pyridyl or substituted or unsubstituted pyrrolyl wherein substituents that can be used for R2, R3 and R4 represent halogen atom, substituted or unsubstituted heterocycle taken among the group consisting of pyridine, pyrrolidine, piperidine, pyrrole, substituted or unsubstituted (C3-C6)-cycloalkyl. Indicated compounds are effective in treatment of impotency that represents one of male sexual dysfunction. Method involves stage of interaction of alkoxybenzoic acid with pyrazoleamine to yield the corresponding compound pyrazoleamide, stage of chlorosulfonation of pyrazoleamide to yield the corresponding chlorosulfonated compound, stage of interaction of chlorosulfonated compound with primary amine R4NH2 wherein R4 has values indicated above, to yield sulfonamide, and stage of intramolecular cyclization of sulfonamide. Invention provides preparing end compounds by economy method with high yields and purity.

EFFECT: improved preparing method, valuable medicinal properties of compounds.

7 cl, 3 ex

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Authors

Joo Moo-Khi

Kim Von-Bae

Chang Min-Sun

Kim Soon-Khoe

Kim Dong-Sung

Bae Chul-Dzun

Kim Jong-Duk

Kim Eun-Kha

Dates

2004-09-20Published

2001-05-18Filed