With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.5908-62-3,1,1-Dioxo-isothiazolidine,as a common compound, the synthetic route is as follows.,5908-62-3
A microwave vial was charged with (5-{7-chloro-6-fluoro-5-[(S)-oxan-4- yl(phenyl)methyl]-5H-pyrido[3,2-b]indol-3-yl}-4-(2H3)methyl-l-methyl-lH-l,2,3- triazole (30 mg, 0.061 mmol), isothiazolidine 1,1-dioxide (11.1 mg, 0.091 mmol), tripotassium phosphate (18.1 mg, 0.085 mmol), Pd2(dba)3 (2.8 mg, 3.0 muiotatauiotaomicron), 2-di-tert- butylphosphino-3,4,5,6-tetramethyl-2′,4′,6′-triisopropyl-l, -biphenyl (2.9 mg, 6.1 mumol), and dry tert-butanol (0.5 mL). The reaction was heated at 84C overnight. It was diluted with water and extracted with ethyl acetate. The organic layer was concentrated and purified by preparative HPLC (Column: XBridge CI 8, 19 x 200 mm, 5-muiotatauiota particles; Mobile Phase A: 5:95 acetonitrile: water with 10-mM ammonium acetate; Mobile Phase B: 95:5 acetonitrile: water with 10-mM ammonium acetate; Gradient: 15-55% B over 15 min, then a 5-min hold at 100% B; Flow: 20 mL/min) to give 2.1 mg (6%). NMR (500 MHz, DMSO) delta 8.61 (s, 1H), 8.11 (m, 1H), 7.96 (s, 1H), 7.64 (m, 2H), 7.45 (m, 1H), 7.35 (m, 2H), 7.28 (m, 1H), 5.91 (m, 1H), 3.9 (m, 5H), 3.77 (m, 1H), 3.52 (m, 3H), 3.29 (m, 1H), 2.55 9m, 2H), 1.78 (m, 1H), 1.35 (m, 2H), 1.1 (m, 1H); LCMS (M+H) = 578.35
The synthetic route of 5908-62-3 has been constantly updated, and we look forward to future research findings.
Reference£º
Patent; BRISTOL-MYERS SQUIBB COMPANY; HAN, Wen-Ching; DEGNAN, Andrew P.; DESKUS, Jeffrey A.; GAVAI, Ashvinikumar V.; GILL, Patrice; SCHMITZ, William D.; STARRETT, John E., Jr.; (193 pag.)WO2016/183115; (2016); A1;,
Thiazolidine – Wikipedia
Thiazolidine – ScienceDirect.com