With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.2510-36-3,3,5-Dimethylisoxasole-4-carboxylic acid,as a common compound, the synthetic route is as follows.
A vial was charged with 3-fluoro-4- [[(3S)-3-methyl- 1,1 -dioxo-6-phenyl-thiazinan-2- ylimethyllaniline hydrochloride (75 mg, 0.19 mmol), 3,5-dimethylisoxazole-4-carboxylic acid (41 mg, 0.29 mmol), triethylamine (0.14 mL, 0.97 mmol) and N,N-dimethylformamide (1 mL), followed by O-(7-azabenzotriazol- 1 -yl)-N,N,N?,N?-tetramethyluronium hexafluorophosphate (92 mg, 0.23 mmol) and the reaction was stirred at room temperature for 2 hours. The reaction was then partitioned between dichloromethane and saturated sodium bicarbonate in water. The organic layer was separated, concentrated and purified by preparative HPLC to give N-[3-fluoro- 4- [[(3S)-3-methyl- 1,1 -dioxo-6-phenyl-thiazinan-2-yllmethyllphenyll -3,5 -dimethyl-isoxazole-4- carboxamide Stereoisomer A (23.6 mg, 0.050 mmol, 26% yield). ?H NMR (400 MHz, DMSO)o 10.22 – 10.18 (s, 1H), 7.67 – 7.60 (m, 1H), 7.51 – 7.44 (m, 3H), 7.44 – 7.34 (m, 4H), 4.54 – 4.46 (m, 2H), 4.39 – 4.33 (m, 1H), 4.17 – 4.07 (m, 1H), 2.57 – 2.52 (s, 3H), 2.47 – 2.39 (m, 1H),2.34- 2.29 (s, 3H), 2.16 -2.06 (m, 1H), 1.90- 1.75 (m, 1H), 1.71 – 1.61 (m, 1H), 1.13 – 1.07 (d, J = 6.8 Hz, 3H); LCMS [M+1j = 472.2.
2510-36-3, As the paragraph descriping shows that 2510-36-3 is playing an increasingly important role.
Reference£º
Patent; F. HOFFMANN-LA ROCHE AG; GENENTECH, INC.; FAUBER, Benjamin; RENE, Olivier; WO2014/202741; (2014); A1;,
Isoxazole – Wikipedia
Isoxazole | C3H3NO – PubChem