摘要 |
<p>PROBLEM TO BE SOLVED: To provide a method which enables high-speed methylation of an spcarbon under a condition of a low-concentration [C] CHI condition applicable to [C] methylation.SOLUTION: A high-speed methylation method comprises cross-coupling, with methyl iodide, a boronic acid ester compound with the carbon at the allyl or benzyl position converted to a boronate ester, in an aprotic polar solvent, e.g. DMF, in the presence of a palladium complex of formula Pd[PRRR](at least one of substituent groups R, Rand Ris an alkyl group) and a base. The aprotic polar solvent preferably contains water. Pd[PRRR]is typically Pd[P(tert-CH)].</p> |