Reference of 1186050-58-7, A common heterocyclic compound, 1186050-58-7, name is 2-Fluoro-6-(2H-1,2,3-triazol-2-yl)benzoic acid, molecular formula is C9H6FN3O2, its traditional synthetic route has been very mature, but the traditional synthetic route has various shortcomings, such as complicated route, low yield, poor purity, etc, below Introduce a new synthetic route.
Compound 9-2 (120 mg, 0.32 mmol), compound 9-3 (77 mg, 0.38 mmol), HATU (182 mg, 0.48 mmol) and DIEA (124mg, 0.96 mmol) were dissolved in 5 mL of DMF, and the mixture was stirred under room temperature for 3 hours. The reaction mixture was poured into aqueous saline and extracted with ethyl acetate (10 mL x 3). The organic phase was combined and washed with water (10 mL x 2) and saturated NaCl solution (10 mL x 2), dried with anhydrous Na2SO4, filtered, and concentrated to obtain a crude product. The crude product was purified with preparative HPLC to give product 9-4 (22 mg, white solid, yield: 21 %). 1H NMR (400 MHz, MeOD) delta= 8.20-7.98 (m, 3H), 7.85-7.72 (m, 1H), 7.71-7.50 (m, 2H), 7.48-7.17 (m, 1H), 7.03-6.75 (m, 1H), 4.87-4.66 (m, 1H), 4.54-4.36 (m, 1H), 4.31-4.05 (m, 1H), 3.86-3.55 (m, 1H), 2.14 (br. s., 1H), 2.08-1.95 (m, 1H), 1.88 (td, J=7.2, 19.8 Hz, 2H), 1.77 (dd, J=11.3, 18.1 Hz, 2H), 1.68-1.54 (m, 1H), 1.53-1.32 (m, 2H)
The synthetic route of 1186050-58-7 has been constantly updated, and we look forward to future research findings.
Reference:
Patent; Shanghai Haiyan Pharmaceutical Technology Co. Ltd.; Yangtze River Pharmaceutical Group Co., Ltd.; HE, Haiying; WU, Songliang; ZHANG, Yang; MA, Biao; CHEN, Yuan; WANG, Yuhe; CHEN, Shuhui; LV, Qiang; LAN, Jiong; LIU, Xing; (54 pag.)EP3115362; (2017); A1;,
1,2,3-Triazole – Wikipedia,
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