| 摘要 |
The invention presents a process for preparing the benzenes 1-substituted with tetrazole groups of the general formula (I): wherein R 1 is hydrogen, t-butyl, phenoxy, phenyl, C1-C6 dialkylamino or trimethylsylyl; R2 is hydrogen or trityl; R3 is alpha-hydroxybenzyl, trimethylsylyl, thiophenyl, thiomethyl, carboxyl, 2 - hydroxyethyl, azide, trimethylstannyl, C1-C6 alkyl, bromine or iodine, starting from aryltetrazole of formula II: where R1 and R2 having the above meaning, are treated with alkyl lithium in an aprotic solvent, at a temperature in the range of - 40 to + 10 degrees C, for 0.5 ... 5 hours, to obtain an ortho-lithiated intermediate which reacts in situ with an electrophylic E1 compound selected from benzaldehyde, trimethylsylyl chloride, phenylsulphide, methylsulphide, carbon dioxide, ethylene oxide, p-toluen sulphonylazide, trimethylstannyl chloride, C1-C6 alkyl chloride, bromine or iodine.
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