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.
Article
in Chinese
| WPRIM
| ID: wpr-845159
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.
Full text:
Available
Index:
WPRIM (Western Pacific)
Language:
Chinese
Journal:
Journal of International Pharmaceutical Research
Year:
2020
Type:
Article
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