1-N-Boc-4-甲氨甲基哌啶合成方法

Synthesis of 1-N-Boc-4-[(Methylamino)methyl]Piperidine

以4-哌啶甲酸为原料,经酯化、还原、(Boc)2O保护、溴代、甲胺化五步反应,以72%的总收率合成了重要药物中间体1-N-Boc-4-甲氨甲基哌啶。合成方法操作简单、收率高。

Using piperidine-4-carboxylic acid as the starting material, and via esterification, reduction, protection with（Boc）20, bromination, methanamination overall five steps, an important pharmaceutical intermediate l-N-Boc-4-[（methylamino）methyl]piperidine was synthesized with total yield of 72 %. The method was a better choice for the industry of the title compound.