ALKYLATING AGENTS AND METHOD FOR 1,4-ADDITIONING AN ALKYL GROUP TO AN ALPHA, BETA-UNSATURATED KETO-COMPOUND

摘要

PCT No. PCT/EP94/01001 Sec. 371 Date Nov. 15, 1995 Sec. 102(e) Date Nov. 15, 1995 PCT Filed Mar. 30, 1994 PCT Pub. No. WO94/22878 PCT Pub. Date Oct. 13, 1994Disclosed is an alkylating agent that contains an aluminum reagent Alk3-m AlLm, in which Alk means a methyl, ethyl, n- or i-propyl, n-, i- or tert-butyl, pentyl, hexyl, heptyl or octyl group, which all can also be branched, L means an ethoxy group, a chlorine or bromine atom, and m is equal to 1 or 2, as an alkyl source or else zinc dimethyl as a methyl source, which contains in addition catalytic amounts of one or more copper(I) and/or copper(II) compounds and one (or more) silyl reagent(s) of general formula IIIR1R2R3SiZ(III),in which R1, R2 and R3 are as defined herein, as well as a process for 1,4-addition of an alkyl group to an alpha , beta -unsaturated ketone or an alpha , beta -double unsaturated ketone or to an alpha , beta -unsaturated aldehyde with use of the agent according to the invention. The alkylating agent yields biologically active compounds in excellent yields and the new alkylating agent/process is distinguished by its environmental compatibility based on a CKW (chlorinated hydrocarbon)-free reaction medium.