反应 #1509653

反应方程式

4-(2-(2-chloro-9-isopropyl-9H-purin-6-ylamino)ethyl)phenol

thianaphthene-3-boronic acid

Cs2CO3

1,3-bis(2,4,6-trimethylphenyl) imidazolium chloride

→

title compound

4-(2-(2-(benzo[b]thiophen-3-yl)-9-isopropyl-9H-purin-6-ylamino)ethyl)phenol

反应条件

后处理

1. 1
   其他The flask was evacuated
2. 2
   workup.ADDITIONwas added
3. 3
   其他The flask was sealed
4. 4
   浓缩The reaction mixture was concentrated
5. 5
   其他purified directly by column chromatography on silica gel
6. 6
   洗涤eluting with hexane/EtOAc (20:1 to 1:4)

实验过程

A flame-dried schlenk flask was charged with 4-(2-(2-chloro-9-isopropyl-9H-purin-6-ylamino)ethyl)phenol (0.62 mmol), thianaphthene-3-boronic acid (0.94 mmol), pd2(dba)3 (0.062 mmol), Cs2CO3 (1.25 mmol) and 1,3-bis(2,4,6-trimethylphenyl) imidazolium chloride (0.125 mmol). The flask was evacuated and backfilled with N2 and anhydrous 1,4-dioxane (2 mL) was added. The flask was sealed and the reaction mixture was stirred at 80° C. for 24 hours. The reaction mixture was concentrated and purified directly by column chromatography on silica gel, eluting with hexane/EtOAc (20:1 to 1:4) to afford the title compound as a yellowish solid.

来源