Application of 131803-48-0 ,Some common heterocyclic compound, 131803-48-0, molecular formula is C8H8BrNO2, its traditional synthetic route has been very mature, but the traditional synthetic route has various shortcomings, such as complicated route, low yield, poor purity, etc., below Introduce a new synthetic route.
To a solution of tert-butyl 4-(N-phenylsulfamoyl)piperazine-1-carboxylate (0.600 g, 1.757 mmol) in N,N-dimethylformide (10 mL) was slowly added sodium hydride (60.00 %, 0.091 g, 2.285 mmol) at the room temperature, and the mixture was stirred for 5 min at the same temperature. The reaction mixture was treated with methyl 6-(bromomethyl)nicotinate (0.485 g, 2.109 mmol), and stirred at the same temperature for additional 16 hr. Then, saturated aqueous sodium bicarbonate solution was added to the reaction mixture, followed by extraction with ethyl acetate. The organic layer was washed with aqueous saturated sodium chloride solution, dried with anhydrous MgSO4, filtered, and concentrated in vacuo. The residue was chromatographed (SiO2, 40 g cartridge; ethyl acetate / hexane = 10 % to 50 %) to give the crude product, which was dissolved in hexane (100 mL), and stirred. The resulting precipitates were collected by filtration, washed by hexane, and dried to give tert-butyl 4-(N-((5-(methoxycarbonyl)pyridin-2-yl)methyl)-N-phenylsulfamoyl)piperazine-1-carboxylate as white solid (0.585 g, 67.9 %).
In the field of chemistry, the synthetic routes of compounds are constantly being developed and updated. I will also mention this compound in other articles. 131803-48-0, Methyl 6-(bromomethyl)nicotinate, other downstream synthetic routes, hurry up and to see.
Reference:
Patent; CHONG KUN DANG PHARMACEUTICAL CORP.; LEE, Jaekwang; HAN, Younghue; KIM, Yuntae; MIN, Jaeki; BAE, Miseon; KIM, Dohoon; JIN, Seokmin; KYUNG, Jangbeen; (191 pag.)WO2017/18805; (2017); A1;,
Pyridine – Wikipedia,
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