496-41-3,With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.496-41-3,Benzofuran-2-carboxylic acid,as a common compound, the synthetic route is as follows.
Trifluoroacetic acid (2 ml) was added to a solution of (S)-1-((6S,7S,9aR)-6- hydroxy-3-oxo-octahydro-pyrrolo[1,2-a]azepin-7-ylcarbamoyl)-3-methyl-butyl]-carbamic acid tert-butyl ester (158 mg, 0.4 mmol) in CH2Cl2 (2 ml) at rt. The reaction mixture was stirred for 1 hr at rt, then was concentrated under the reduced pressure. After drying under the vacuum, the residue was dissolved in DMF (3 ml) followed by the addition of benzofuran-2-carboxylic acid (76 mg, 0.47 mmol), hydroxybenztriazole (69 mg, 0.51 mmol), 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide HCl (97 mg, 0.51 mmol), and diisopropylethylamine (0.18 ml, 1.03 mmol). The reaction mixture was stirred for overnight at rt, and DMF was removed under the reduced pressure, then was diluted with EtOAc (70 ml), washed with cold 1N HCl (50 ml), sat’d NAHC03 (50 ml), and brine (50 ml), dried over magnesium sulfate, filtered, concentrated in vacuo by rotary evaporation, and chromatographed on silica gel (2% to 5% MeOH/CH2Cl2) to yield the title compound (116 mg, 66% for two steps); 1H NMR (CDCl3)]: delta 0.99 (d, J = 6.3 Hz, 3H), 1.01 (d, J = 6.3 Hz, 3H), 1.50-1.96 (m, 8H), 2.10-2.20 (m, 1H), 2.38-2. 53 (m, 2H), 3.19 (d, J = 14.2 Hz, 1H), 3.66-3.75 (m, 1H), 3.81-3.93 (m, 2H), 4.10 (d, J = 15.2 Hz, 1H), 4.58-4.65 (m, 1H), 6.66 (brs, 1H), 7.01 (d, J = 8.1 Hz, 1H), 7.31-7.56 (m, 4H), 7.70 (d, J = 7.6 Hz, 1H); LCMS: 442.2 (MH+).
The synthetic route of 496-41-3 has been constantly updated, and we look forward to future research findings.
Reference£º
Patent; SMITHKLINE BEECHAM CORPORATION; WO2003/103574; (2003); A2;,
Benzofuran – Wikipedia
Benzofuran | C8H6O – PubChem