Азапропазон

Химические свойства

Nearly colorless, crystalline solid.

Использование

Cyclo-oxygenase inhibitor; analgesic; anti-inflammatory.

Определение

ChEBI: A member of the class of benzotriazines that is 1,2-dihydro-1,2,4-benzotriazine bearing a dimethylamino substitutent at position 3 and a methyl substituent at position 7 and in which the nitrogens at positions 1 and 2 are both acylated by a carboxy group o propylmalonic acid.

Всемирная организация здравоохранения(ВОЗ)

Azapropazone, which has anti-inflammatory, analgesic and antipyretic activity, was introduced in 1970 for the treatment of rheumatic disorders. Although sometimes classified as a pyrazolone derivative, the relationship with this group of compounds has been disputed and classification as a benzotriazine derivative might be preferable. Although, to date, it has not been associated with blood dyscrasias, some regulatory authorities have applied the same rigorous restrictions to its indications as they have applied to pyrazolone derivatives. The World Health Organization was informed that as of December 1987 azapropazone was available in some 27 countries.

Опасность

Nausea, vomiting, abdominal pain, gastric ulcers; moderately toxic.

Профиль безопасности

Moderately toxic by ingestion,intraperitoneal and intravenous routes. When heated todecomposition it emits toxic fumes of NOx.

Синтез

Synthesis: a mixture of 1,2-dihydro-3-dimethylamino-7-methylbenzotriazine, diethyl propylmalonate, and sodium ethoxide in xylene is heated over a period of time to 150 ?C, cooled, and acidified to give the desired product.