| 摘要 |
The invention relates to a method for production of a 3- hydrocarbyl-3-cephem derivative with formula I and pharmaceutically acceptable acid addition salts, basic salts and esters thereof, <IMAGE> in which formula R1 is 1-alkenyl, 1-polyalkenyl, 1- alkynyl or a carbocyclic or heterocyclic aryl and Q is hydrogen or R-CO-, where R is an organic group with 1-20 carbon atoms, or Q is a trialkylsilyloxycarbonyl or triarylsilyloxycarbonyl group, which can be substituted, or trialkylsilyl or triarylsilyl. According to the method, a 3-trifluoromethanesulphonyloxy-3-cephem is used as the reactant in a relatively polar, aprotic solvent and this reactant is brought into contact with at least an equimolar amount of a hydrocarbyltrialkylstannane, in the presence of about 1-10 mol% of a palladium compound, about 3-30 mol% of a phosphine reagent and about 0-7 molar equivalents of a metal halide, after which the 3- hydrocarbyl-3-cephem compound obtained is recovered from the reaction mixture. The invention also relates to intermediate products which are used in the method. |
