| 摘要 |
1. The method of producing precursors of 2-n-butylo-4-chloro-1-{[2'-(2H-tetrazole-5-yl)-1,1'-biphenyl-4-yl]methyl}-5-hydroxymethyl-1H-imidazole with the general formula :I where: P refers to triphenylmethyl, t-butyl, C1-C4-alkoxymethyl, methyl-thiomethyl, phenylo-C1-C4-alkoxymethyl, p-methoxybenzyl, 2,4,6-trimethyl-benzyl, 2-(trimethyl-silyl)ethyl, tetrahydropiranyl, piperonyl or benzenesulphonyl, through the reaction of aryl halides and arylboronic acids in the presence of a base and a complex palladium compound. Characterized in that: The compound with the general formula II, where P has the meaning defined above, while R1a> and R1b> refer independently to an chlorine atom, a bromine atom, C1-C4-alkoxyl or hydroxyl, or R1a> and R1b> together with an atom of boron form the configuration: IMAGE>, where A refers to phenyl or (CH2)n, where n is within the range 2 through 4 - this compound is subjected to reaction with the electrophilic compound with the general formula III, where: X refers to an atom of bromine, an atom of iodine, methane-sulphonyl-oxyl, toluene-sulphonyl-oxyl, fluorine-sulphonyl-oxyl or tri-fluorine-methane-sulphonyl-oxyl. The reaction is carried out in an organic solvent, preferably toluene, tetra-hydro-furane or di-ethoxy-methane, in the presence of a complex palladium compound as a catalyst and a base. The content of water should not exceed 3 molar parts per 1 molar part of the compound with the formula II. The reaction is carried out for 1-30 hours at the temperature range between room temperature and 150 degrees C. The resultant compound with the formula I may finally be purified and/or re-crystallised. |
