総説および総合論文
迅速な臨床導入に向けたE2212原薬の効率的製法の開発
2020 年 78 巻 8 号 p. 760-769
詳細
2020 年 78 巻 8 号 p. 760-769
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 could be established and successfully scaled-up to hundred kilogram scale. For a rapid delivery of drug substance containing Z-isomer for preclinical safety studies, successful scale-up of photo-isomerization of an olefin under flow system is also presented.
