反応 #342512

反応方程式

Intermediate 6

2-{4-[(tert-butoxycarbonyl)amino]piperidin-1-yl}ethyl methanesulfonate

Quinolin-2(1H)-one

sodium hydride

Intermediate 141

tert-butyl {1-[2-(7-fluoro-2-oxoquinoxalin-1(2H)-yl)ethyl]piperidin-4-yl}carbamate

2-{4-[(tert-butoxycarbonyl)amino]piperidin-1-yl}ethyl methanesulfonate

→

product

収率 35.0%

tert-Butyl {1-[2-(2-oxoquinolin-1(2H)-yl)ethyl]piperidin-4-yl}carbamate

収率 35.0%

溶媒

dichloromethane

methanol

反応条件

実験手順

Quinolin-2(1H)-one (250 mg, 1.7 mmol) was deprotonated with sodium hydride (60% in oil, 70 mg, 1.7 mmol) and alkylated with 2-{4-[(tert-butoxycarbonyl)amino]piperidin-1-yl}ethyl methanesulfonate (Intermediate 6) (1.7 mmol) as described for Intermediate 141. Chromatography on silica gel with 0-5% methanol in dichloromethane gave 220 mg (35%) of product as a colorless solid.

出典