Application of 10244-24-3, In the chemical reaction process,reaction time,type of solvent,can easily affect the result of the reaction, thereby determining the yield and properties of the reaction product.An updated downstream synthesis route of 10244-24-3 as follows.
Example 8: Preparation of Trianion of 5-bromo-4-(trifluoromethyl)pyridin-2-amine using 3.5 Equivalents of Isopropylmagnesium chloride, lithium chloride complexA reactor was charged with 5-bromo-4-(trifluoromethyl)pyridin-2-amine (1.000 g, 4.149 mmol) and tetrahydrofuran (7.72 ml). The mixture was sitrred for 10 minutes. The mixture was cooled to 0 C within 30 minutes. lsopropylmagnesiumcloride lithium chloride 1 .3M in THF (6.383 ml,8.298 mmol) was continuously added within a time period of 1.5 hours at 0 C. An additional1.5 equivalents of isopropylmagnesiumcloride lithium chloride 1 .3M in THF (4.788 ml, 6.224 mmol) was continuously added within a time period of 1 .5 hours at 0 C. An additional 0.5 equivalents of isopropylmagnesiumcloride lithium chloride 1 .3M in THF (1 .596 ml, 2.075 mmol) was continuously added within a time period of 1 hour at 0 C. The product was the trianion of 5-bromo-4-(trifluoromethyl)pyridin-2-amine, as determined by HPLC and LCMS.Example 9: Preparation of 5-(2,6-Di-4-morpholinyl-4-pyrimidin-4-yl)-4- (trifluoromethyl)pyridin-2-amine (Compound A)The compound 4,4?-(6-chloropyrimidine-2,4-diyl)dimorpholine (0.40g, 1.405 mmol), 1,1?- Bis(diphenylphosphino)ferrocene (0.040g, 0.070 mmol) and Palladium acetate (0.016g, 0.070 mmol) and 2 mL of tetrahydrofuran were placed in an inertized reactor. The reactor is evacuated to 100 mbar and flushed with nitrogen two times. lsopropylmagnesiumcloride lithium chloride 1 .3M in THF (1.405 mmol) was added at 30 C followed by an equivalent amount of the trianion of 5-bromo-4-(trifluoromethyl)pyridin-2-amine (1.405 mmol). The suspension was stirred for 0.5 hours. The product was 5-(2,6-Di-4-morpholinyl-4-pyrimidin-4-yl)-4- (trifluoromethyl)pyridin-2-amine, as determined by HPLC and LCMS.
These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route,10244-24-3, its application will become more common.
Reference:
Patent; NOVARTIS AG; FLUBACHER, Dietmar; BIERI, Nicole; ACEMOGLU, Murat; MICHEL, Pascal; MOSE, Rasmus; STETTLER, Hans; TESTA, Maria Caterina; BROZIO, Joerg; SCHAEFER, Frank; WO2014/64058; (2014); A1;,
Pyrimidine | C4H4N2 – PubChem,
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