With the rapid development and complex challenges of chemical substances, the synthesis of new drugs is usually one of the most effective ways to increase yield.302964-08-5, name is 2-((6-Chloro-2-methylpyrimidin-4-yl)amino)-N-(2-chloro-6-methylphenyl)thiazole-5-carboxamide, molecular formula is C16H13Cl2N5OS, molecular weight is 394.2783, as common compound, the synthetic route is as follows.Safety of 2-((6-Chloro-2-methylpyrimidin-4-yl)amino)-N-(2-chloro-6-methylphenyl)thiazole-5-carboxamide
A mixture of 2-(6-chloro-2-methylpyrimidin-4-ylamino)-N-(2-chloro-6-methyl phenyl) thiazole- 5 -carboxamide compound of formula-2 (50 gm), 2-(piperazin-l-yl)ethanol compound of formula-3 (82.5 gm) & 1 ,2-propanediol (750 ml) is expelled with nitrogen for 30 minutes. N,N- diisopropylethylamine (43.6 ml) was added to the reaction mixture and heated the reaction mixture to 115-120C. Stirred the reaction mixture for 8 hours at the same temperature. Cooled the reaction mixture to 25-30C and stirred for 6 hours at the same temperature. Filtered the precipitated solid and washed with 1 ,2-propanediol. Methanol (1300 ml) was added to the obtained wet compound and heated the reaction mixture to 65-70C. Stirred the reaction mixture for 2 hours at the same temperature. Filtered the reaction mixture at 65-70C and washed with methanol. Cooled the filtrate to 25-30C and stirred for 2 hours at the same temperature. Filtered the precipitated solid, washed with methanol and dried to get the title compound. Yield: 38 gm; HPLC Purity: 99.57%, 0.01% (N-Oxide impurity), 0.09% (Deshydroxyethyl dasatinib); PXRD pattern of the obtained compound depicted in figure-5.
At the same time, in my other blogs, there are other synthetic methods of this type of compound,302964-08-5, 2-((6-Chloro-2-methylpyrimidin-4-yl)amino)-N-(2-chloro-6-methylphenyl)thiazole-5-carboxamide, and friends who are interested can also refer to it.
Reference:
Patent; MSN LABORATORIES PRIVATE LIMITED; THIRUMALAI RAJAN, Srinivasan; ESWARAIAH, Sajja; MADHUSUDHAN, Gutta; SEETHA RAMA SARMA, Peri; KHALIL AHAMED, Mogal; (38 pag.)WO2017/2131; (2017); A1;,
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia