联系我们 / CONTACT US
0591-83441193
地址：福州市仓山区进步路25号
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.
福建省微生物研究所
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