PURPOSE: To prepare substituted benzoxazoles, benzothiazoles, oxazolopyridines and thiazolopyridines having leukotriene biosynthesis inhibiting performance.
CONSTITUTION: The compd. of formula I [X is O or S; Y and Z are C or N, where they are not simultaneously N; R1 and R2 are H, an alkyl, halo, CF3 CN, alkoxy or CO2R7 (R7 is H or an alkyl) or the like; R3 is methyl, cyclohexyl, phenyl, NO2, 1-piperidinyl, imidazole, dialkylamine or the like; R4 is CO2R16 (R16 is an alkyl), C(O) NR17R18 (R17 and R18 are H, an alkyl or the like), phenyl, 2-imidazole or the like; R5 and R6 are H or methyl; (n) is 0 to 2], such as DL- N-(benzothiazol-2-yl)phenylalanine ethyl ester. The compd. is obtd. by bringing a compd. of the formula II (Hal is an halogen) to react with an amine of formula III in the presence of a basic catalyst in an inert solvent.
ADAMS JULIAN (US)
MIAO CLARA K (US)
FARINA PETER (US)
