Related Products of 634468-96-5, 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 634468-96-5 as follows.
General procedure: 2-Chloro-4-iodotoluene (250muL, 1.78mmol), 1-Boc-piperazine (398mg, 2.14mmol), Pd2(dba)3 (40.8mg, 0.045mmol), Xantphos (103mg, 0.178mmol) and potassium tert-butoxide (280mg, 2.50mmol) were dissolved in toluene (5mL) and heated at reflux for 16h under N2. The reaction was then concentrated and dissolved in EtOAc (20mL), filtered through celite and washed with additional EtOAc (50mL). The organic layer was washed with water (2×20mL) and brine (2×20mL), then dried with Na2SO4 and concentrated in vacuo. The crude residue was then purified by column chromatography (100% CyHex to 10% EtOAc/CyHex) to obtain the protected intermediate as an oil (436mg, 79%). MS, m/z=311 (100) [M+H]+, 313 (30). The intermediate was then dissolved in a 1:3 mixture of TFA/DCM (4mL) and stirred at 20C for 1h. The solvent was then evaporated in vacuo and the crude residue dissolved in EtOAc (10mL) which was then successively washed with a 10% NaHCO3 solution (10mL), water (10mL) and brine (10mL). The organic layer was then dried with Na2SO4 and concentrated in vacuo to obtain 106 as a solid (288mg, 97%).
These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route,634468-96-5, its application will become more common.
Reference:
Article; Blackmore, Timothy R.; Jacobson, Jonathan; Jarman, Kate E.; Lewin, Sharon R.; Nguyen, William; Purcell, Damian F.; Sabroux, Helene Jousset; Sleebs, Brad E.; European Journal of Medicinal Chemistry; vol. 195; (2020);,
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