反応 #8678

反応方程式

1-(2-fluorobenzyl)-1H-pyrazolo[3,4-b]pyridine-3-carboximidamide

1-(2-Fluorobenzyl)-1H-pyrazolo[3,4-b]pyridine-3-carboximidamide

diethyl 2-(8-oxa-3-azabicyclo[3.2.1]oct-3-yl)malonate

Diethyl 2-(8-oxa-3-azabicyclo[3.2.1]oct-3-yl)malonate

→

2-[1-(2-Fluorobenzyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]-5-(8-oxa-3-azabicyclo-[3.2.1]oct-3-yl)-4,6-pyrimidinediol

溶媒

toluene

反応条件

後処理

1. 1
   ろ過The solid is then filtered off with suction
2. 2
   洗浄washed with diethyl ether
3. 3
   その他dried in vacuo

実験手順

0.50 g (1.11 mmol) of 1-(2-fluorobenzyl)-1H-pyrazolo[3,4-b]pyridine-3-carboximidamide (example I, step 5) are suspended in 40 ml of toluene. Then 1.40 g (5.16 mmol) of diethyl 2-(8-oxa-3-azabicyclo[3.2.1]oct-3-yl)malonate from step 5 are added. The mixture is stirred at 140° C. overnight. The solid is then filtered off with suction, washed with diethyl ether dried in vacuo.

出典