Development of an Efficient Manufacturing Process for E2212 toward Rapid Clinical Introduction

Autor:	Francis G. Fang, Kazuhiro Yoshizawa, Atsushi Kamada, Taiju Nakamura, Masaaki Matsuda, Katsuya Tagami, Nobuaki Sato, Takeo Sasaki, Yongbo Hu, George A. Moniz, Minetaka Isomura, Yoshihiro Nishikawa, Gordon D. Wilkie, Daiju Hasegawa, Yorihisa Hoshino, Kazato Inanaga, Toshiyuki Uemura
Rok vydání:	2019
Předmět:	Safety studies 010405 organic chemistry Manufacturing process Computer science business.industry Organic Chemistry 010402 general chemistry 01 natural sciences 0104 chemical sciences Flow system γ secretase Physical and Theoretical Chemistry Process engineering business
Zdroj:	Organic Process Research & Development. 23:603-613
ISSN:	1520-586X 1083-6160
DOI:	10.1021/acs.oprd.8b00444
Popis:	Process studies of E2212 (1) toward rapid clinical introduction are described. Through comprehensive route-finding studies and optimization of key condensation and cyclization steps, a racemate-based manufacturing route was established and successfully scaled-up to the hundred kilogram scale. For the rapid delivery of a drug substance containing the Z isomer for preclinical safety studies, the successful scale-up of the photoisomerization of an olefin in a flow system is also presented.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_________::46a6b7869f9ea3690bb1a0225426216e https://doi.org/10.1021/acs.oprd.8b00444 Zobrazit plný text záznamu