反应 #742310

反应方程式

1-{(R)-1-[9-[(2R,3R,4S R)-3,4-dihydroxy-5-(2H-tetrazol-5-yl)-tetrahydro-furan-2-yl]-6-(2,2-diphenyl-ethylamino)-9H-purin-2-yl]-pyrrolidin-3-yl}-3-pyridin-3-yl-urea

potassium carbonate

DMF

→

titled compound

1-{(R)-1-[9-{(2R,3R,4S,5R)-3,4-Dihydroxy-5-[2-(2-hydroxy-ethyl)-2H-tetrazol-5-yl]-tetrahydro-furan-2-yl}-6-(2,2-diphenyl-ethylamino)-9H-purin-2-yl]-pyrrolidin-3-yl}-3-pyridin-3-yl-urea

反应条件

后处理

1. 1
   过滤The mixture is then filtered
2. 2
   浓缩the filtrate is concentrated in vacuo
3. 3
   其他Purification of the crude product by C-18 reverse phase column chromatography
4. 4
   洗涤eluting with acetonitrile

实验过程

A solution of 1-{(R)-1-[9-[(2R,3R,4S R)-3,4-dihydroxy-5-(2H-tetrazol-5-yl)-tetrahydro-furan-2-yl]-6-(2,2-diphenyl-ethylamino)-9H-purin-2-yl]-pyrrolidin-3-yl}-3-pyridin-3-yl-urea in DMF is treated with potassium carbonate followed by 3-bromoethanol and stirred at RT for 18 hours. The mixture is then filtered and the filtrate is concentrated in vacuo. Purification of the crude product by C-18 reverse phase column chromatography eluting with acetonitrile:water (0.1% TFA) (gradient 0-100% acetonitrile) to affords the titled compound.

来源