Researchers who often do experiments know that organic synthesis is a process of preparing more complex target molecules from simple raw materials through one or more chemical reactions. Generally, it requires fewer steps, and cheap raw materials. 364-12-5, name is 5-Bromo-2-iodobenzotrifluoride, A new synthetic method of this compound is introduced below., name: 5-Bromo-2-iodobenzotrifluoride
A vial containing 4-bromo-l-iodo-2-(trifluoromethyl)benzene was charged with potassium phosphate (0.130 g, 0.614 mmol), followed by a solution of N-(2,4- dimethoxybenzyl)-l-methyl-3-(4,4,5,5-tetramethyl- 1,3, 2-dioxaborolan-2-yl)-N-( 1 ,2,4- thiadiazol-5-yl)-lH-indole-6-sulfonamide (Intermediate H) (0.100 g, 0.175 mmol) and PdCl2(dppf)-CH2Cl2 (0.014 g, 0.018 mmol) in 1 mL of DMF. The vial was sealed and placed in a shaker block. The block was shaken for three hours at 85 C. The solution was filtered, washed with DMF and concentrated. The resulting solid was treated with a solution of TFA (0.270 mL, 3.51 mmol) in 1 mL of DCM. The vial was shaken at room temperature for two hours. The solution was concentrated and purified via reverse phase HPLC (8 min. gradient elution 15 to 75% ACN/H20, 0.1% TFA modifier) to afford 3-(4- bromo-2-(trifluoromethyl)phenyl)-l-methyl-N-(l,2,4-thiadiazol-5-yl)-lH-indole-6- sulfonamide as an off-white solid.
The basis of chemical reaction formula synthesis, the synthesis route is composed of some specific reactions and combined according to certain logical thinking. We look forward to the emergence of more reaction modes in the future.
Reference:
Patent; DINEEN, Thomas; MARX, Isaac, E.; NGUYEN, Hanh, Nho; WEISS, Matthew; AMGEN INC.; WO2013/25883; (2013); A1;,
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com