Fmoc-N-甲基-L-苯丙氨酸的微波辅助合成

The Synthesis of Fmoc-N-methyl-L-phenylalanine with Microwave-assisted

以Fmoc保护的L-苯丙氨酸为起始原料,经恶唑烷酮中间体,在三氟乙酸和无水AlCl3共同催化下,三乙基硅烷还原得到Fmoc保护的N-甲基L-苯丙氨酸,总收率82%。反应过程中,采用微波辐射代替传统的加热方式,缩短了时间,提供了产率,三氟乙酸和无水三氯化铝共同催化体系避免了副产物Fmoc-Tic-OH的生成,该方法优化了生产工艺,缩短了反应时间,节约了原料。

Fmoc-protected N-methyl-L-phenylalanine was synthesized under the presence of trifluoroacetic acid and anhydrous aluminum chloride as catalyzer and the triethylsilane as reduction,in which the Fmoc-protected L-phenylalanine was used as original material,passing though the genarated intermediate 5-oxazolidinone with microwave assisted heating method.The result showed that using the microwave assisted heating method,the reaction time greatly reduced and the mean total yield increased to 82%,and the composite catalyzer of trifluoroacetic acid and anhydrous aluminum chloride could avoid generating the by-product Fmoc-Tic-OH and save original material.