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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 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.

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