Synthesis and syntehtic process optimization of mTOR protein inhibitor Torin2
10.13220/j.cnki.jipr.2020.07.010
- VernacularTitle: mTOR 蛋白抑制剂Torin2 的合成与合成工艺优化
- Author:
Shi-Xu WANG
1
Author Information
1. College of Chemistry Chemical Engineering and Environmental Engineering, Liaoning Shihua University
- Publication Type:Journal Article
- Keywords:
MTOR inhibitor;
Process optimization;
Torin2
- From:
Journal of International Pharmaceutical Research
2020;47(7):549-554
- CountryChina
- Language:Chinese
-
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 and Conclusion: 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.
