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. 141738-80-9, name is 3-Chloro-4-iodobenzotrifluoride, A new synthetic method of this compound is introduced below., category: iodides-buliding-blocks
Step A: Diboron pinacol ester (329.61mg, 1.30mmol, 1.10eq) and tetrakis(triphenylphosphine)platinum(73.53mg, 59.09umol, 0.05eq) were added to a solution of compound 10 (200.00mg, 1.18mmol, 1.00eq) in 2-methyltetrahydrofuran(5.00mL), the reaction solution was purged three times with nitrogen and stirred at 70C under nitrogenatmosphere for 5 hours. After the reaction solution was cooled to 0C, compound 5 (285.58mg, 945.27umol, 0.80eq),cesium carbonate (769.97mg, 2.36mmol, 2.00eq), 0.4mL water, 5mL 2-methyltetrahydrofuran and dichlorobis(triphenylphosphine)palladium (41.47mg, 59.08umol, 0.05eq) were added, then the reaction solution was purged three timeswith nitrogen and stirred at 20C under nitrogen atmosphere for 12 hours. Then 2-chloro-4-trifluoromethyl iodobenzene(717.09mg, 2.34mmol, 2.00eq), aqueous potassium hydroxide (4M, 1.46mL, 5.00eq), dichlorobis(triphenylphosphine)palladium (41.06mg, 58.50umol, 0.05eq) and 10mL 2-methyltetrahydrofuran were added to the reaction solution,which was subsequently purged three times with nitrogen. After stirring at 70C under nitrogen atmosphere for 12 hours,the reaction solution was filtered through celite, concentrated and purified by silica gel column chromatography(PE:EA=40:1 to 15:1) to give the compound 47 as a yellow jelly (738.00mg), which was directly used in the next step.
The synthetic route of 141738-80-9 has been constantly updated, and we look forward to future research findings.
Reference:
Patent; Luoxin Biotechnology (Shanghai) Co., Ltd.; Shandong Luoxin Pharmaceutical Group Stock Co., Ltd.; LU, Jianyu; DING, Charles Z.; HU, Lihong; HE, Huijun; CHEN, Shuhui; DONG, Jiaqiang; WANG, Tie-lin; (124 pag.)EP3434668; (2019); A1;,
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com