An automated-flow microreactor system for quick optimization and production: application of 10- and 100-gram order productions of a matrix metalloproteinase inhibitor using a Sonogashira coupling reaction |
| |
Authors: | Atsushi Sugimoto Md Taifur Rahman |
| |
Institution: | a Synthetic Chemistry, CMC Development Laboratories, Shionogi & Co., Ltd, Amagasaki, Hyogo 660-0813, Japan b Department of Chemistry, Graduate School of Science, Osaka Prefecture University, Sakai, Osaka 599-8531, Japan |
| |
Abstract: | Sonogashira coupling reaction leading to a matrix metalloproteinase inhibitor was investigated using an automated microreactor system, which is a sequential temperature- and flow rate-programed reaction evaluation system. By repeating the use of this computer-controlled system four times, we were able to determine the optimal conditions and quickly apply them to a 10 g scale synthesis using the same microreactor system. The optimal conditions were also applied to a 100 g scale production by using another microflow system composed of a T-shaped micromixer (200 μm id) and a stainless tube reactor (2000 μm id and 20 m length). Total time spent for both optimization and production was as short as 50 h. |
| |
Keywords: | |
本文献已被 ScienceDirect 等数据库收录! |
|