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.
324.0 mg (2 mmol) of benzofuran-2-carboxylic acid was suspended in 5 mLs of methylene chloride. The flask was flushed with argon for 10 minutes before injection of 0.4 mL (4 mmol) oxalyl chloride. Two drops of dimethylformamide were injected and furious bubbling began. The sealed vessel was continuously flushed with argon and vented for 2 hours at room temperature. 10 mLs of sieve dried ethanol was slowly injected and allowed to stir for an additional hour. Volatiles were removed under vacuum and the crude intermediate was resuspended in 5 mLs ethanol. To this solution was added 250 mg (5 mmol) of hydrazine water salt. The reaction was refluxed for 3 hours to give the corresponding hydrazide. Volatiles were removed under vacuum and the product suspended in 10 mLs of ethanol. From here the reaction proceeded as described in Series 1 General Procedure to yield 369.1 mg of dry product (72% yield). ?H NMR (400 MHz, DMSO): 10.26 (d, J 6.0 Hz, 1H),7.78 (d, J 8.0 Hz, 1H), 7.66 (d, J 8.4 Hz, 1H), 7.54 (s, 1H), 7.49-7.45 (m, 1H), 7.36-7.32 (m, 1H), 5.16-5.13 (m, 1H), 2.84-2.79 (m, 2H), 1.48-1.41 (m, 2H), 1.39-1.33 (m, 2H), 0.90 (t, J= 7.2 Hz,3H); ?3CNMR(100MHz,DMSO): 157.7, 154.7, 148.7, 127.5, 127.2, 124.2, 123.1, 112.2, 109.6, 51.2, 30.2, 20.3, 14.4. [(m+H)/z = 233.25]. (2254) purity 98.8%, tR 11.53 mins.
496-41-3, The synthetic route of 496-41-3 has been constantly updated, and we look forward to future research findings.
Reference£º
Patent; MUSC FOUNDATION FOR RESEARCH DEVELOPMENT; CHOU, Chung-Jen, James; MCCLURE, Jesse; ZHANG, Cheng; INKS, Elizabeth; (68 pag.)WO2018/71740; (2018); A1;,
Benzofuran – Wikipedia
Benzofuran | C8H6O – PubChem