Chromone compounds

摘要

Chromone compounds having the structure (I) (I') wherein R is aryl, substituted aryl, thienyl, furyl or pyridyl, Y is hydroxy (lower) alkylene, R1 is hydrogen, lower alkyl, aryl, substituted aryl or a heterocyclic group, R2 is hydrogen or lower alkoxy, Y1 is lower alkylene or hydroxyl (lower) alkylene, Z is oxygen or sulfur and R3 is hydrogen, lower alkyl, aryl, substituted aryl, or ar(lower)alkyl have anti-allergic activity and are useful in the treatment of asthma. Compounds of the structure [I] are prepared by reacting (II) wherein Y' is hydroxy (lower) alkylene whose hydroxy group is optimally protected or a reactive derivative of [II] with a carboxylic acid of the formula R-COOH in the presence of a basic catalyst. The resulting compound is then reacted with an acid. Compounds of the structure [I] are prepared by reacting the compound (IV) with the compound X-Y1'-Z-R3' wherein X is an acid residue, Y' is lower alkylene or hydroxy (lower) alkylene whose hydroxy group is optionally protected by a protective group, R3' is hydrogen, lower alkyl, aryl, substituted aryl, or ar(lower)alkyl and Z is defined above. When R3' is hydrogen, -Z-R3' is optionally protected by a protective group. The resultant compound is subjected to an elimination reaction when Y' is a protected group or when -Z-R3' is protected to split off the protective group.