Synthesis and syntehtic process optimization of mTOR protein inhibitor Torin2 / 国际药学研究杂志
Journal of International Pharmaceutical Research
; (6): 549-554, 2020.
Artigo
em Chinês
| WPRIM (Pacífico Ocidental)
| ID: wpr-845159
Biblioteca responsável:
WPRO
ABSTRACT
Objective:
To synthesize the mammalian target of sirolimus(mTOR)inhibitor Torin2 and optimize the synthetic process.Methods:
Starting from p-bromoaniline, the target product was obtained through amino bonding, cyclization, chlorination, bonding with 3-aminotoluene ring, oxidation, cyclization and Suzuki reaction. The synthetic conditions for the key intermediates 3 and 8 as well as the final product Torin2 were optimized by the orthogonal experiment. Results andConclusion:
The structures of the intermediates and the target compound were confirmed by MS and 1H NMR data. The total yield of the target compound synthesis increased from 3% to 18%, and no column chromatography was required for the target compound separation and purification, which thus makes it suitable for industrial production.
Texto completo:
Disponível
Base de dados:
WPRIM (Pacífico Ocidental)
Idioma:
Chinês
Revista:
Journal of International Pharmaceutical Research
Ano de publicação:
2020
Tipo de documento:
Artigo