Analyzing the synthesis route of 24340-77-0

The synthetic route of 24340-77-0 has been constantly updated, and we look forward to future research findings.

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.24340-77-0,4-Bromoisothiazole,as a common compound, the synthetic route is as follows.

(B) (2E)-Ethyl 3-(4-(isothiazol-4-yl)pyridin-3-yl)acrylate A mixture of (2E)-ethyl 3-(4-(tributylstannyl)pyridin-3-yl)acrylate (33 mg), 4-bromoisothiazole (17.41 mg), Pd(Ph3P)4 (8.18 mg), copper(I) iodide (2.70 mg), cesium fluoride (21.50 mg) and DMF (1.5 mL) was stirred under nitrogen atmosphere at 100 C. for 13 hours. Likewise, a mixture of (2E)-ethyl 3-(4-(tributylstannyl)pyridin-3-yl)acrylate (497 mg), 4-bromoisothiazole (262 mg), Pd(Ph3P)4 (123 mg), copper(I) iodide (40.6 mg), cesium fluoride (324 mg) and DMF (10 mL) was stirred under nitrogen atmosphere at 100 C. for 13 hours. The reaction mixtures were combined, and the insoluble matter was then filtered. The filtrate was diluted with ethyl acetate (20 mL), water (10 mL) and saturated aqueous sodium bicarbonate solution (10 mL), and the aqueous layer was extracted with ethyl acetate. The extract was washed with water and brine and then dried over anhydrous sodium sulfate, and the solvent was distilled off under reduced pressure. The residue was purified by silica gel column chromatography (ethyl acetate/hexane) to obtain the title compound (222 mg). MS: [M+H]+ 260.9.

The synthetic route of 24340-77-0 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Takeda Pharmaceutical Company Limited; HIRAYAMA, Takaharu; FUJIMOTO, Jun; CARY, Douglas Robert; OKANIWA, Masanori; HIRATA, Yasuhiro; (147 pag.)US2017/44132; (2017); A1;,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com