Reference of 356068-93-4,Some common heterocyclic compound, 356068-93-4, name is (Z)-5-((5-Fluoro-2-oxoindolin-3-ylidene)methyl)-2,4-dimethyl-1H-pyrrole-3-carboxylic acid, molecular formula is C16H13FN2O3, 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.
To a stirred solution of compound 109 (0.5 g, 1.67 mmol) in THF(150 mL) at00C was added HOBt (0.34 g, 2.8 mmol), triethylamine (0.6 mL, 4.18 mmol),ECDI HCl (0.48 g, 2.8 mmol) and compound 202 (0.6 g, 3.33 mmol) successively. The mixture was stirred overnight at room temperature, evaporated to remove solvent, diluted with water (50 mL), brine (50 mL) and saturated sodium bicarbonate solution (50 mL). The pH of solution was adjusted to 11-12 with 1OM NaOH. The mixture was filtered, washed with water, dried to obtain crude yellow solid 203 (550 mg, 69%). LCMS: 478 [M+l]+, 1H NMR (DMSO-J6): delta 2.40 (s, 3H), 2.43 (s, 3H), 3.63 (m, 2H),3.82 (s, 3H), 4.20 (t,2H), 6.92 (m, 2H), 7.07 (d, 2H), 7.70 (m, 2H), 7.84(s, 1H),7 .91 (d, 2H), 10.88 (s, IH), 13.68 (s, IH).
The synthetic route of 356068-93-4 has been constantly updated, and we look forward to future research findings.
Reference:
Patent; CURIS, INC.; WO2008/33747; (2008); A2;,
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