CHEMBRDG-BB 6625984 synthesis

Yield:98555-49-8 86.6%

Reaction Conditions:

with nitric acid;acetic acid at 20 - 25;

Steps:

Intermediate: methyl (R)-1-(3-amino-5-cyano-4-phenol)-pyrrolidine-3-carboxylic acid methyl ester (G)

Step 1: Dissolve compound G1 (20.0g, 99.5mmol) in 150ml of glacial acetic acid, add concentrated nitric acid (12.9g, 139.3mmol) dropwise within 30 minutes at room temperature, and stir the reaction at room temperature overnight. Use petroleum Dilute with ether (1.5 L), filter, wash the filter cake with petroleum ether, and dry in vacuo to obtain compound G2 (21.2 g, yellow solid) with a yield of 86.6%.

References:

CN113248492,2021,A Location in patent:Paragraph 0352; 0382-0384