Related Products of 761440-16-8 , The common heterocyclic compound, 761440-16-8, name is 2,5-Dichloro-N-(2-(isopropylsulfonyl)phenyl)pyrimidin-4-amine, molecular formula is C13H13Cl2N3O2S, its traditional synthetic route has been very mature, but the traditional synthetic route has various shortcomings, such as complicated route, low yield, poor purity, etc., below Introduce a new synthetic route.
To 500L enamel reactor was added 80.6kg of isopropanol,12.4 kg of the compound 1-dihydrochloride obtained in Example 1 and 14.7 kg of the compound 3 obtained in Example 6,Heated to reflux, the reaction 24 hours. The reaction solution was cooled to 10 C, stirred for 3 hours,filter.The wet filtered product was added enamel reactor,99.2 kg of isopropanol and 13.0 kg of purified water were added,Reflux stir until solids are clear.Control temperature not lower than 85 ,99.2 kg of isopropanol was added dropwise.Slowly cooled to 20 ,Stir for 2 hours and filter.The wet filtered product was added to the enamel reactor again,Add 99.2 kg of isopropanol and 13.0 kg of purified water and stir under reflux until the solid is clear.Controlled at a temperature not lower than 85 C, 99.2 kg of isopropanol was added dropwise.Slowly cooled to 20 C, stirred for 2 hours, filtered, washed with isopropanol.The filtered wet product was vacuum dried at 55 C for 16 hours,A 16.4 kg yellow solid (Compound 4, ceritinib dihydrochloride) was obtained in a yield of 67% and a purity of 99.9%.
The synthetic route of 761440-16-8 has been constantly updated, and we look forward to future research findings.
Reference:
Patent; Shanghai Xingtai Pharmaceutical Technology Co., Ltd.; Liu Xuejun; Hong Huiyi; Chen Xiaodong; (12 pag.)CN106854200; (2017); A;,
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia