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928775-04-6

1-(5-Bromopyridin-2-yl)pyrrolidin-2-one synthesis

4synthesis methods
-

Yield:928775-04-6 62%

Reaction Conditions:

with potassium carbonate in acetonitrile at 20;Inert atmosphere;

Steps:

C

intermediate 2h: l-(5-(2-(2-(cyclopropylamino)thiazol-4-yl)phenyl)pyridin-2- yl)pyrrolidin-2-one from l-(5-bromopyridin-2-yl)pyrrolidin-2-one which was synthesized from 5-bromopyridin-2-amine as follows:In a 250 mL round bottom flask were introduced successively under Ar: 5- bromopyridin-2-amine (10 g, 57.8 mmol), K2C03 (32.0 g, 231 mmol) and dry MeCN ( 1 15 mL). To this suspension was added at once 4-bromobutanoyl chloride (10 mL, 86.7 mmol) and the RM was stirred at RT overnight.The RM was filtered and the solid washed with MeCN. The filtrate was concentrated and the residue taken up in EtOAc and diluted with water. The organic layer was then washed with aqueous HC1 0.5M, dried and concentrated in vacuo to give 8.67g (62%) of title product as a white solid,

References:

WO2011/151434,2011,A1 Location in patent:Page/Page column 53