110-91-8

58757-38-3

64614-49-9

General procedure for the synthesis of (6-chloro-3-pyridine)-4-morpholinemethanone from 6-chloro-3-pyridinecarbonyl chloride and morpholine: To a solution of 6-chloro-3-pyridinecarbonyl chloride (0.540 g, 3.07 mmol) in methylene chloride (10 mL) was added sequentially morpholine (0.294 g, 1.1 eq.) and triethylamine (940 μL, 2.2 eq.). The reaction mixture was stirred at room temperature overnight. The progress of the reaction was monitored by thin-layer chromatography (TLC), and after confirming that 6-chloro-3-pyridinecarbonyl chloride was completely consumed and the mass spectrum showed the molecular ion peak (M+) of the target product, an aqueous post-treatment was performed. The crude product (6-chloro-3-pyridinyl)-4-morpholinemethanone obtained was directly used in the next step of the reaction without further purification. After aqueous treatment, 0.610 g of the crude product was obtained in 88% yield.