文献类型：会议论文

英文题名：Process optimization in the synthesis of sertindole using alkylimidazolium-based ionic liquids as solvents for N-alkylation

作者：Li, Wen[1]; Wang, Panan[1]; Zhang, Wenya[1]; Ma, Xiaoqing[1]; Zhu, Jiangtian[2]

第一作者：Li, Wen

通讯作者：Li, W.

机构：[1] School of Chemical Engineering and Energy, Zhengzhou University, Zhengzhou 450001, China; [2] Department of Culture and Communication, Henan University of Economics and Law, Zhengzhou 450002, China

第一机构：School of Chemical Engineering and Energy, Zhengzhou University, Zhengzhou 450001, China

通讯机构：[1]School of Chemical Engineering and Energy, Zhengzhou University, Zhengzhou 450001, China

会议论文集：Proceedings - 2012 International Conference on Biomedical Engineering and Biotechnology, iCBEB 2012

会议日期：May 28, 2012 - May 30, 2012

会议地点：Macau, China

语种：英文

外文关键词：Biomedical engineering - Biotechnology - Ionic liquids - Ketones - Optimization - Solvents - Synthesis (chemical)

摘要：Sertindole is a well-known antipsychotic drug. Its chemical name is 1-[2 -[4-[5 - chloro - 1- (4 - fluorophenyl) - 1 - H - indol - 3 - yl] - 1-piperidinyl] ethyl] - 2 - imidazolidinone. Sertindole was originally produced via the 1 - (2 - chloroethyl) - 2 - imidazolidinon with N-alkylation of 5 - chloro - 1 - (4 - fluorophenyl) - 3 - (piperidine - 4 - yl) in dole in methyl isobutyl ketone for 12h. This step required significant optimization to improve yield and reproducibility. Under common conditions, the solvent play an important role in the N-alkylation reaction. Ionic liquid is a new kind reaction medium which have environmentally friendly characteristic. Basic ionic liquid [bmin]OH was found to be a suitable solvent for the N-alkylation. A robust production process of Sertindole was obtained through the solvent optimization. The modification and process improvement was scaled-up successfully to batch sizes of > 1 kg. ? 2012 IEEE.