With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.5198-88-9,2-Bromothiazole-4-carboxylic acid,as a common compound, the synthetic route is as follows.
2-Bromo-l,3-thiazole-4-carboxylic acid (200.0 mg, 961 pmol), TEA (671 pL, 4.80 mmol), HATU (547.0 mg, 1.44 mmol) and (R)-N-((S)-l,3-dihydrospiro[indene-2,4′- piperidin]-l-yl)-2-methylpropane-2-sulfmamide (352.0 mg, 1.15 pmol, synthesized via Step a of Example 120) were placed into DMF(l5 mL). The reaction mixture was evacuated and refilled 3 times using N2, and the reaction mixture was stirred at 25 C for 1 hour. The mixture was then diluted with EtOAc (100 mL) and the mixture was washed with H20 (30 mL x 5), brine (50 mL), dried over anhydrous Na2S04, filtered and concentrated to give a residue. The residue was purified by silica gel chromatography (ethyl acetate in petroleum ether = 0% to 80%) to afford (S)-N-((S)- ‘-(2-bromothiazole-4-carbonyl)- 1 ,3- dihydrospiro[indene-2,4’-piperidin]-l-yl)-2-methylpropane-2-sulfmamide (458 mg, 96% yield) as yellow oil. LC-MS (ESI+) m/z: 498.0 (M+H)+.
The synthetic route of 5198-88-9 has been constantly updated, and we look forward to future research findings.
Reference£º
Patent; RELAY THERAPEUTICS, INC.; D.E. SHAW RESEARCH, LLC; TAYLOR, Alexander, M.; LESCARBEAU, Andre; KELLEY, Elizabeth, H.; SHORTSLEEVES, Kelley, C.; WALTERS, W., Patrick; MURCKO, Mark, Andrew; MCLEAN, Thomas, H.; GUNAYDIN, Hakan; GIORDANETTO, Fabrizio; THERRIEN, Eric; (607 pag.)WO2019/183367; (2019); A1;,
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