METHOD OF PREPARING BIPHENYLTETRAZOLE COMPOUNDS AND INTERMEDIATES THEREOF

摘要

Disclosed is a method of preparing biphenyltetrazole compounds of the general formula (II) wherein: P is triphenylmethyl, tertiary-butyl, C1-C4 alkoxymethyl, methylthiomethyl, phenyl C1-C4 alkoxymethyl, p-methoxybenzyl, 2,4,6 trimethylbenzyl, 2-(trimethylsilyl)ethyl, tetrahydropyranyl, piperonyl, or benzenesulfonyl; and Q is H, C1-C4 alkyl, hydroxymethyl, tri[(C1-4)organo]silyloxymethyl, hydroxy C1-C4 alkyl, formyl, C1-C4 acyl, C1-C4 alkoxycarbonyl, or other formula defined in the claim 1; which method can be characterised in that a tetrazolylphenylboronic acid derivative of the general formula (I), wherein P is as defined, R1a and R1b are each independently chlorine, bromine, C1-C4 alkoxy or hydroxy or the both residues can be taken together with B to form a cyclic structure D, where A is phenyl, or (CH2)n, where n is 2 - 4, reacts with an electrophile having the formula Q-phenylen-X wherein Q is as defined, X is bromine, iodine, methanesulfonyloxy, toluenesulfonyloxy, fluorosulfonyloxy, or trifluorome thanesulfonyloxy in the presence of a metal catalyst, a base and a coupling solvent for one to thirty hours at a temperature ranging from room temperature to 150 degrees Celsius. Intermediates of the formula (I) for the synthesis of the formula (II). Compounds of the general formula (II) for the production of the AII receptor antagonists.