Application of 40724-47-8, In the chemical reaction process, reaction time, type of solvent, can easily affect the result of the reaction, thereby determining the yield and properties of the reaction product. An updated downstream synthesis route of 40724-47-8 as follows.
[0216] In a microwave tube was placed ethyl 2-(5-fluoro-3-(4,4,5,5-tetramethyl-1,3,2- dioxaborolan-2-yl)- 1H-indol- 1 -yl)thiazole-4-carboxylate (114 mg, 0.15 mmol, ?55percent purity), 4-(bromomethyl)benzenesulfonamide (49.9 mg, 0.200 mmol), and Pd(Ph3P)4 (17.33 mg,0.0 15 mmol). The tube was sealed and air was removed and re-filled with N2 (2-3 times). A mixture of toluene (0.75 ml, ratio: 2.500)/EtOH (0.3 ml, ratio: 1.000) was added, and then 2 N Na2CO3(aq) (0.3 mL, 0.6 mmol, 4 equiv) was added. The mixture was stirred at 80 ¡ãC (preheated) for 2 h. The organic layer was separated, and the aqueous layer was extracted with EtOAc (2 mL x 3). The combined organic layer was dried (Na2504) and filtered. After removal of the solvent, the product was purified by silica gel chromatography using 20-50percent EtOAc/hexane as the eluent to give ethyl 2-(5-fluoro-3-(4-sulfamoylbenzyl)-1H-indol-1- yl)thiazole-4-carboxylate (47 mg, 0.102 mmol, 68.2percent yield) as a white solid.
According to the analysis of related databases, 40724-47-8, the application of this compound in the production field has become more and more popular.
Reference:
Patent; THE UNITED STATES OF AMERICA AS REPRESENTED BY THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES; VANDERBILT UNIVERSITY; MALONEY, David J.; JADHAV, Ajit; BANTUKALLU, Ganesha Rai; BRIMACOMBE, Kyle Ryan; MOTT, Bryan T.; YANG, Shyh Ming; URBAN, Daniel Jason; HU, Xin; SIMEONOV, Anton; KOUZNETSOVA, Jennifer L.; WATERSON, Alex Gregory; SULIKOWSKI, Gary Allen; KIM, Kwangho; CHRISTOV, Plamen; JANA, Somnath; (387 pag.)WO2016/109559; (2016); A2;,
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