Application of 637031-88-0, 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 637031-88-0 as follows.
To a mixture of 3-methyl-4-[3-(trifluoromethyl)-[1,2,4]triazolo[4,3-a]pyrazin-6-yl]phenol (80 mg, 0.27 mmol), 3,3-difluorocyclobutanol (88.17 mg, 0.82 mmol) and Ph3P (142.64 mg, 0.54 mmol) in THF (2 mL) was added DEAD (94.7 mg, 0.54 mmol) at 0 C under N2. Then the mixture was stirred at 70 C for 16 hours. The mixture was concentrated to give the crude product. The crude product was purified by Prep-HPLC (Waters Xbridge (150 mm x 25 mm, 5 _) A = H20 (10 mM NH4HCO3) and B = CH3CN; 43-73% B over 6 minutes) to give the product (4.22 mg, 11.0 mmol) as a solid. 1H NMR (400MHz, CDC13) _ = 9.57 (d, 1H), 8.13 (s, 1H), 7.38 (d, 1H), 6.84 – 6.80 (m, 1H), 6.77 (dd, 1H), 4.78 -4.66 (m, 1H), 3.20 – 3.09 (m, 2H), 2.86 -2.74 (m, 2H), 2.41 (s, 3H). LCMS R, = 1.16 min in 2.0 min chromatography, 10-80AB, purity 100%, MS ESI calcd. for Ci7H14F5N40 [M+H]+ 385.1, found 385.1.
These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route,637031-88-0, its application will become more common.
Reference:
Patent; PRAXIS PRECISION MEDICINES, INC.; REDDY, Kiran; MARTINEZ BOTELLA, Gabriel; GRIFFIN, Andrew, Mark; MARRON, Brian, Edward; (364 pag.)WO2018/98499; (2018); A1;,
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