With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.24621-73-6,4-Chloro-1H-indole-2-carboxylic acid,as a common compound, the synthetic route is as follows.,24621-73-6
Step 1. 4-Chloro-N-methoxy-N-methyl-1H-indole-2-carboxamide A mixture of 4-chloro-1H-indole-2-carboxylic acid (from Ryan Scientific, 1.0 g, 5.1 mmol), O-(benzotriazol-1-yl)-N,N,N’,N’-tetramethyluronium hexafluorophosphate (2.9 g, 7.7 mmol) and triethylamine (3.6 mL, 26 mmol) in N,N-dimethylformamide (15 mL) was stirred at room temperature for 10 minutes. N,O-Dimethylhydroxylamine hydrochloride (0.75 g, 7.7 mmol) was added and the resulting suspension was stirred at room temperature overnight. The mixture was quenched with water and then extracted with EtOAc. The combined organic layers were dried over MgSO4, concentrated and purified on silica gel (eluting with 0-35% EtOAc in hexane) to give the desired product (0.35 g, 29%). LCMS calculated for C11H12ClN2O2(M+H)+: m/z=239.1; Found: 239.1.
24621-73-6 4-Chloro-1H-indole-2-carboxylic acid 90561, aindole-building-block compound, is more and more widely used in various fields.
Reference£º
Patent; Li, Yun-Long; Combs, Andrew P.; US2011/312979; (2011); 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