Studies On The Synthesis Of Nefiracetam And Ranolazine

Nefiracetam, N-(2, 6-Dimethylphenyl)-2-(2-oxo-l-pyrrolidinyl)acetamide, is a new kind of pyrrolidone derivatives, which can be used as an efficient drug for therapy of Vascular'sdementia (VD) and Alzheimer's disease (AD). The clinical evidences show its distinguished function in improving the circulation and oxygen supply of brain. The drug has been developed and is in its clinical experiment period by the First Pharmaceutical Company of Japan. It has a bright application future, but there is still no report about its production in china until now.This paper focuses on the synthesis of Nefiracetam based on composed analysis of literature's work. A simple and reasonable synthetic method, which is available for the industry use, was found after studying the reaction condition and mechanism.The structures of the target compound and the intermediates were confirmed by MS, IR, 1H NMR spectra and elemental analysis.This synthesis route mainly has three improvements comparing with the literature methods.1.Using PhCH3 as the solvent instead of CH2Cl2, which is volatile and expensive.2.Using CH3ONa as base instead of NaNH2 (NaH), which is expensive and dangerous in transport.3.Using Na2CO3 to absorb HC1 instead of Et3N.The advantage of the method is: moderate synthesis condition, simple procedure, the cheap agents, the low cost of production and the good stability.