反応 #172095

反応方程式

2,6-dichloro-5-fluoronicotinamide

(R)-benzyl-1-(1-aminopropyl)cyclopropylcarbamate hydrochloride salt

DIPEA

→

(R)-benzyl 1-(1-(6-chloro-5-cyano-3-fluoropyridin-2-ylamino)propyl)cyclopropylcarbamate

収率 44.8%

溶媒

NMP

EtOAc

反応条件

後処理

1. 1
   洗浄was washed brine
2. 2
   その他dried
3. 3
   濃縮concentrated

実験手順

To a solution of 2,6-dichloro-5-fluoronicotinamide (233 mg, 1.22 mmol) in NMP (5.0 mL) was added (R)-benzyl-1-(1-aminopropyl)cyclopropylcarbamate hydrochloride salt (350 mg, 1.23 mmol) and DIPEA (0.434 mL, 2.44 mmol). After heated at 80° C. for 4 h, the mixture was diluted with EtOAc, organic layer was washed brine, dried and concentrated to give (R)-benzyl 1-(1-(6-chloro-5-cyano-3-fluoropyridin-2-ylamino)propyl)cyclopropylcarbamate (220 mg).

出典