tert-Butyl 3-oxoazetidine-1-carboxylate synthesis

Yield:398489-26-4 98.11%

Reaction Conditions:

with oxygen;nitric acid;3-carboxy proxyl in ethyl acetate at 50; for 8 h;Reagent/catalyst;Temperature;Solvent;

Steps:

1; 2; 3; 4; 5; 6 Example 4:

In a 250ml four-necked flask equipped with mechanical stirring, put 20g of N-Boc-3-hydroxyazetidine, 80g of ethyl acetate, 0.50g of 98% nitric acid, 3-carboxy-2,2,5,5-tetramethyltetrahydropyrrole nitroxide radical 0.40g, stir to dissolve, vacuum, oxygen replacement, react with oxygen at 50°C for 8 hours, after the reaction is complete, put sodium hydroxide water into the reaction flask to adjust the pH to 6-7 , Filter, wash the filtrate with drinking water, extract the water layer with ethyl acetate, combine the ethyl acetate layers, distill off the ethyl acetate under reduced pressure, crystallize from heptane, and collect N-Boc-3-carbonylazetidine 19.50 g (yield 98.11%).

References:

CN113582901,2021,A Location in patent:Paragraph 0025-0036