反应 #742313

反应方程式

carbonic acid (1S,4R)-4-(2,6-dichloro-purin-9-yl)-cyclopent-2-enyl ester ethyl ester

Intermediate 1

carbonic acid (1S,4R)-4-(2,6-dichloro-purin-9-yl)-cyclopent-2-enyl ester ethyl ester

(1H-pyrazol-4-yl)-methanol

triphenyl phosphine

→

title compound

{1-[(1S,4R)-4-(2,6-Dichloro-purin-9-yl)-cyclopent-2-enyl]-1H-pyrazol-4-yl}-methanol

溶剂

THF

反应条件

后处理

1. 1
   其他The solvent is removed in vacuo
2. 2
   其他the crude product is purified by chromatography on silica eluting with MeOH/DCM (1:25)

实验过程

A mixture comprising carbonic acid (1S,4R)-4-(2,6-dichloro-purin-9-yl)-cyclopent-2-enyl ester ethyl ester (Intermediate 1) (1.00 g, 2.92 mmol), (1H-pyrazol-4-yl)-methanol (preparation shown below) (0.34 g, 3.50 mmol) and triphenyl phosphine (0.115 g, 0.44 mmol) in deoxygenated THF (10 mL) under an inert atmosphere of argon is treated with tris(dibenzylideneacetone)dipalladium (0) (0.13 g, 0.15 mmol) and stirred at 50° C. for 1 hour. The solvent is removed in vacuo and the crude product is purified by chromatography on silica eluting with MeOH/DCM (1:25) to yield the title compound.

来源