Synthetic Route of 4152-90-3, 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 4152-90-3 as follows.
A solution of tert-butyl (trans)-2-(6-bromopyridin-3-yl)cyclopropylcarbamate (Intermediate E, 350 mg, 1.118 mmol), 3-chlorobenzylamine (237 mg, 1.677 mmol), Sodium tert-butoxide (161 mg, 1.677 mmol) in 1,4-dioxane (7 mL) was degassed for 30 min, tris(dibenzylidene acetone)dipalladium(0) (51 mg, 0.055 mmol), 4,5-Bis(diphenyl phosphino)-9,0-dimethyl xanthene (193 mg, 0.335 mmol) was added and heated for 4 h at 80¡ã C. After completion, the solvent was removed, the residue was poured into ice cold water (10 mL) and extracted with EtOAc (2*20 mL). The combined extracts were washed with water (10 mL), brine (10 mL), dried over anhydrous Na2SO4, filtered and evaporated. The crude residue was purified by flash chromatography to give tert-butyl (trans)-2-(6-(3-chlorobenzylamino) pyridin-3-yl)cyclopropyl carbamate (100 mg, yield: 24percent) as white solid.
According to the analysis of related databases, 4152-90-3, the application of this compound in the production field has become more and more popular.
Reference:
Patent; Laria, Julio Castro-Palomino; Fyfe, Matthew Colin Thor; Pedemonte, Marc Murtinell; Munoz, Alberto Ortega; Valls Vidal, Nurla; US2013/289076; (2013); A1;,
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