Synthesis of 2-Morpholine-2-phenylacetic acid derivatives based on Petasis reaction
Phenylglycine is a naturally occurring amino acid,which is an important chemical raw material and widely used in food additives,pharmaceutical intermediates and other fine chemicals.At present,phenylglycine is mainly prepared by traditional methods such as Bucher-Bergs method and 2-halophenylacetic acid amination method.In recent years,research on a new green and efficient synthesis method of phenylglycine and its derivatives has received much attention.This study presents the first one-pot synthesis of 2-morpholine-2-phenylacetic acid derivatives of phenylglycine derivatives using the Petasis reaction.It was found that dichloromethane was used as the reaction solvent and the reaction was stirred at 40℃for 16 h to produce 2-morpholine-2-phenylacetic acid derivatives in high yield;using this process condition,a series of novel derivatives were synthesized and their structures were characterized by nuclear magnetic resonance spectroscopy in this study.Compared with the conventional method,the Petasis reaction can achieve high selectivity for the target amino acids under mild and green conditions.This study provides a new pathway for the industrial production of 2-morpholine-2-phenylacetic acid derivatives and a new way for the development of novel 2-morpholine-2-phenylacetic acid derivatives and their new functional materials.