With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.399-67-7,7-Fluoro-1H-indole-2-carboxylic acid,as a common compound, the synthetic route is as follows.
To a solution of 7-fluoroindole carboxylic acid (500 mg, 2.79 mmol, available from, for example, Matrix Scientific) in DMF (5 mL) was added potassium carbonate (771 mg, 11.2 mmol) followed by bromoethane (521 DL, 6.98 mmol). The reaction mixture was heated at 60 C for 2 h then further bromoethane (521 DL, 6.98 mmol) and potassium carbonate (771 mg, 11.2 mmol) were added. The reaction mixture was heated at 60 C for a further 2 h then concentrated under reduced pressure to give around 2 g of crude material as a beige solid.The material was suspended in a solution of THF (20 mL), water (20 mL) and MeOH (5 mL) then LiOH monohydrate (401 mg, 9.56 mmol) was added. The reaction mixture was stirred at rt for 16 h then concentrated under reduced pressure. The resulting crude product was treated with 2N HC1 (20 mL, aqueous), and the resulting beige solid filtered under reduced pressure then washed with water then further dried under reduced pressure to give the title compound as a beige solid (436 mg, 75%).LCMS (formic) MH+ = 208.0, Rt 1.03 mm
399-67-7, The synthetic route of 399-67-7 has been constantly updated, and we look forward to future research findings.
Reference：
Patent; GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED; AMANS, Dominique; ATKINSON, Stephen, John; BARKER, Michael, David; CAMPBELL, Matthew; DIALLO, Hawa; DOUAULT, Clement; GARTON, Neil, Stuart; LIDDLE, John; RENAUX, Jessica, Fanny; SHEPPARD, Robert, John; WALKER, Ann, Louise; WELLAWAY, Christopher, Roland; WILSON, David, Matthew; (284 pag.)WO2016/185279; (2016); A1;,
Indole alkaloid derivatives as building blocks of natural products from?Bacillus thuringiensis?and?Bacillus velezensis?and their antibacterial and antifungal activity study
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles