反应 #159328

反应方程式

(3R)—N-(8-azabicyclo[3.2.1]octan-3-yl)-3-(5-cyanopyridin-2-ylamino)pyrrolidine-1-carboxamide

i-Pr2NEt

methanesulfonyl chloride

→

title compound

收率 58.6%

(3R)-3-(5-cyanopyridin-2-ylamino)-N-(8-(methylsulfonyl)-8-azabicyclo[3.2.1]octan-3-yl)pyrrolidine-1-carboxamide

收率 58.6%

溶剂

HOAc

MeOH

CH2Cl2

反应条件

后处理

1. 1
   其他purified by prep HPLC

实验过程

To a stirred solution of (3R)—N-(8-azabicyclo[3.2.1]octan-3-yl)-3-(5-cyanopyridin-2-ylamino)pyrrolidine-1-carboxamide (18 mg, 0.053 mmol) and i-Pr2NEt (0.075 mL, 0.4 mmol) in CH2Cl2 (1 mL) was added methanesulfonyl chloride (0.008 mL, 0.10 mmol). The mixture was stirred overnight at rt, diluted with HOAc (0.1 mL) and MeOH (0.9 mL) and purified by prep HPLC to afford the title compound (13 mg, 58%). LC-MS Method 1 tR=1.1 min, m/z=419; 1H NMR (CD3OD) [selected resonances] 2.93 (s, 3H), 4.47 (m, 1H), 6.78 (d, 1H), 7.77 (d, 1H), 8.40 (s, 1H)

来源