5-oxopyrrolidine-2-carbaldehyde synthesis

Yield:62400-90-2 71%

Reaction Conditions:

with Dess-Martin periodane in dichloromethane at 20; for 1 h;Inert atmosphere;Cooling with ice;

Steps:

21.1 First step Synthesis of 5-carbonylpyrrolidine-2-carboxaldehyde 21b

Under nitrogen protection,The compound 5-(hydroxymethyl)pyrrolidin-2-one 21a (1.15 g, 10.0 mmol) was dissolved in dichloromethane (50 mL).DMP (5.1 g, 12.0 mmol) was added portionwise in an ice water bath, and the mixture was allowed to react to room temperature for 1 hour.Filtration, the filtrate was washed with saturated sodium sulfite solution, dried over anhydrous sodium sulfate, filtered, concentrated and purified by column chromatography.To give the title compound 21b (0.8g, 7.1mmol), 71% yield.

References:

CN109897011,2019,A Location in patent:Paragraph 0582-0586