反応 #41137

反応方程式

1-tert-butyl-5-chloro-1H-pyrazole-4-carboxylic acid adamantan-2-ylamide

pyrrolidin-3-ol

→

1-tert-butyl-5-(3-hydroxy-pyrrolidin-1-yl)-1H-pyrazole-4-carboxylic acid adamantan-2-ylamide

収率 22.0%

溶媒

N-methylpyrrolidinone

反応条件

後処理

1. 1
   その他sealed vial under microwave irradiation for 4 hr
2. 2
   その他the crude product was purified by reverse phase HPLC

実験手順

A mixture of 1-tert-butyl-5-chloro-1H-pyrazole-4-carboxylic acid adamantan-2-ylamide (Example 36, 101 mg; 0.30 mmol) and pyrrolidin-3-ol (+/−) (0.25 mL; 3.0 mmol) in N-methylpyrrolidinone (1 mL) was heated to 250° C. in a sealed vial under microwave irradiation for 4 hr. The mixture was allowed to cool to room temperature and the crude product was purified by reverse phase HPLC to provide 1-tert-butyl-5-(3-hydroxy-pyrrolidin-1-yl)-1H-pyrazole-4-carboxylic acid adamantan-2-ylamide (25 mg, 22%) as an off white solid. ES-HRMS m/e calcd for C22H35N4O2 (M+H+) 358.2602, found 358.2602.

出典