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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

✍ Scribed by Atsushi Sugimoto; Takahide Fukuyama; Md. Taifur Rahman; Ilhyong Ryu


Publisher
Elsevier Science
Year
2009
Tongue
French
Weight
699 KB
Volume
50
Category
Article
ISSN
0040-4039

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✦ Synopsis


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 lm id) and a stainless tube reactor (2000 lm id and 20 m length). Total time spent for both optimization and production was as short as 50 h.