Copyright © 2024 福建省微生物研究所 版权所有 网站建设:中企动力福州 闽ICP备10006540
地址: 福州市仓山区进步路25号 办公室电话: 0591-83441193、83476798
科技管理科电话: 0591-83309157、83586273 传真: 0591-83441193 邮箱: fim_cn@163.com
福建省微生物研究所
友情链接:
科研成果
SCIENTIFIC PAYOFFS
A New Method for Synthesis of Nolatrexed Dihydrochloride
{Author}: Xueqing Zhao, Fei Li , Weiping Zhuang, Xiaowen Xue, Jingming Zhou,Dongsheng Fang
{Journal}: Organic Process Research & Development
{Year}: 2010
{Volume}: 14
{Issue}: 2
{Pages}: 346-350
{Abstract}: A new synthetic method for nolatrexed dihydrochloride (thymitaq) has been developed. The synthesis was accomplished in three steps featuring the direct conversion of the starting 4-bromo-5-methylisatin into the methyl anthranilate by potassium peroxydisulfate/sodium methoxide. In the final Ullmann reaction potassium carbonate was employed in place of sodium hydride, and the amount of copper catalysts was significantly reduced. Moreover, sodium sulfide solution was utilized to efficiently remove copper under approximately neutral conditions instead of hydrogen sulfide/methanol under strongly acidic conditions. By means of these modifications, nolatrexed dihydrochloride was ensured to be prepared in good yield and high purity.