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Methyl 4-[(Morpholin-4-yl)carbonyl]benzoate synthesis

9synthesis methods
-

Yield:6724-90-9 98.2%

Reaction Conditions:

with triethylamine in dichloromethane at 0 - 20; for 3 h;Inert atmosphere;

Steps:

5.1

General procedure: Under Ar protection, azetidine hydrochloride (2.12 g, 22.7 mmol),100 mL of dichloromethane and Et3N (10.5 mL, 75.55 mmol) were placed in a 250 mL round bottom flask, and a solution of compound 1b (3.0 g, 15.11 mmol) in 100 mL of dichloromethane was slowly added dropwise at 0 ° C.After the dropwise addition, the reaction system was transferred to room temperature for 3 hours.The reaction was detected by TLC. The organic phase was passed through a 1mol / L hydrochloric acid aqueous solution,It was washed with saturated aqueous NaHCO3 solution and saturated brine, and dried over anhydrous Na2SO4.Concentration under reduced pressure gave Intermediate 2b as a white solid, 3.1 g, yield 93.9%.

References:

CN110759889,2020,A Location in patent:Paragraph 0159; 0197; 0201-0203