PRODUCTION OF 3-ACYLAMINO-6-PHENYLOXY-7-ALKYLSULFONYLAMINO-4H-1-BENZOPYRAN-4-ONE DERIVATIVE OR ITS SALT
PURPOSE:To industrially obtain the subject compound useful as an antiinflammatory agent, etc., in a high yield by reacting a specific benzene derivative with a halogenating agent, aminating the obtained compound, reacting the aminated compound with a specific compound and subsequently cyclizing the...
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Zusammenfassung: | PURPOSE:To industrially obtain the subject compound useful as an antiinflammatory agent, etc., in a high yield by reacting a specific benzene derivative with a halogenating agent, aminating the obtained compound, reacting the aminated compound with a specific compound and subsequently cyclizing the obtained compound. CONSTITUTION:A benzene derivative of formula I [R is (halogenated) phenyl; R is lower alkyl] is reacted with a halogenating agent, and the obtained compound of formula II (X is halogen) is subjected to am aminatination reaction comprising reaction with hexamethylene tetramine and hydrolysis of the reactional product. The obtained compound salt of formula III is reacted with a compound of formula IV [R 1s (halogen-substituted)acyl] or its reactive derivative, and the produced compound of formula V or its salt is cyclized in the presence of a cyclization condensation agent such as N,N- dimethylformamide dimethylacetal to obtain the objective compound of formula V1. |
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