ES431300A1 - Benzoxazoles - Google Patents

Abstract

A method of preparing a benzoxazole derivative of formula I: ** (See formula) ** Where the -CR1R2R3 radical is in the 5- or 6- position of the bensoxazole nucleus, R4 is a phenyl radical optionally substituted in any usable position by one or more C1-6 alkylsulfonyl, halogen, C1-6 alkyl, C1-6 alkoxy, C1-6 haloalkyl, nitro, C2-7 acyl, hydroxy, amino, C1-6 alkylamino, or C2-7 acylamino or optionally substituted at two adjacent positions by methylene or ethylenedioxy, R3 is one of the radicals. ** (See formula) ** where R5 and R6 are independently hydrogen, C1-6alkyl or hydroxyC1-6alkyl, R1 and R2 are independently hydrogen or C1-6; or R3 is a nitrile radical, carboxy or a salt, ester, amido, or the hydroxamic acid derivative thereof, or hydroxymethyl or an ester thereof R1 is hydrogen, halogen, or C1-6 alkyl, and R2 is halogen, hydroxy, amino, C1-6 acoxy, C2-7 acylozi, C1-6 alkylamino, C1-6 dialkylamino, C2-7 acylamino or N-C1-6 alkyl C2-7 acylamino, a process comprising the cyclization of a compound of formula: ** (See formula) ** where V, W and Z are respectively the radicals R1, R2 and R3 or, independently, they can be radicals that are respectively convertible into the radicals R1, R2 and R3 and either X is hydrogen or the radical R4CO- and Y is H2N- or X is hydrogen and Y is the radical R4CO-NH- or R4CH = N-, the cyclization being carried out in the case where X is hydrogen and Y is H2N-, in the presence of a cyclizing agent capable of yielding the radical R4 required and when one or more of the radicals V, W and Z in the resulting compound are not the same as the radicals R1, R2 and R3, respectively, converting said radicals V, W and Z into radicals R1, R2 and R3 in the conventional way. (Machine-translation by Google Translate, not legally binding)