Some tips on 2510-36-3

2510-36-3 3,5-Dimethylisoxasole-4-carboxylic acid 75636, aIsoxazoles compound, is more and more widely used in various fields.

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.,2510-36-3

Example 1; 3,5-Dimethyl-isoxazole-4-carboxylic acid [2-methyl-4-(2(2S)-methyl- [1 ,3′(3 ‘ S)]bipyrrolidinyl- 1 ‘-yl)-phenyl] -amide; 2-Methyl-4-(2(2S)-methyl-[l,3′(3’S)]bipyrrolidinyl-r-yl)-phenylamine (330 mg, 1.15 mmol) was dissolved in DCM (6 mL) and DMF (2 mL), and the solution was cooled to an ice- water bath. To this solution was added powdered 3,5-dimethyl-isoxazole-4-carboxylic acid (168.9 mg, 1.38 mmol, 1.2 equiv.), N-methylmorpholine (280 mg, 3 equiv.), 1- hydroxylbenzotriazole (HOBT) (0.162 g, 1.19 mmol, 1.3 equiv.), sequentially, and finally EDC HCl (0.228 g, 1.19 mmol, 1.3 equiv. ). The resultant clear brown solution was stirred at r.t. overnight. TLC (10% MeOH in DCM) and LC/MS showed that the reaction was complete and the product peak (368) was detected. The reaction was quenched with saturated aqueous sodium bicarbonate solution (3 mL) and 3 mL of DCM. The two layers were separated, and the aqueous layer was extracted with DCM (5 mLx2). The combined DCM extracts were washed with sodium bicarbonate (5 mL), and brine (5 mL), dried (anhydrous potassium carbonate), filtered, and concentrated in vacuo to get a crude product which was purified on a silica gel column (25 g of silica gel) on Analogix to get the title compound as a tan solid, 200 mg (49% yield).LCMS: Rx = 1.54 minutes, MS: 383 (M+H).1H NMR (CDCl3, 300MHz), delta (ppm): 7.44 (m, IH), 6.92 (bs, IH), 6.40 (bs, IH), 6.39 (bs, IH), 3.50 (m, IH), 3.4-3.2 (m, 4H), 3.00 (m, IH), 2.78 (m, IH), 2.66 (bs, 3H), 2.48 (bs, 3H), 2.5 (m, IH), 2.26 (s, 3H), 2.18 (m, IH), 2.00 (m, 2H), 1.79 (m, 2H), 1.48 (m , IH), 1.14 (d, 6.3 Hz, 3H).

2510-36-3 3,5-Dimethylisoxasole-4-carboxylic acid 75636, aIsoxazoles compound, is more and more widely used in various fields.

Reference£º
Patent; SANOFI-AVENTIS; WO2009/52062; (2009); A1;,
Isoxazole – Wikipedia
Isoxazole | C3H3NO – PubChem