反应 #1880976

ord-cc4cbf8d6a6c491aba97605cfc8840b4

反应方程式

C#C[C@H]1O[C@@H](n2cnc3c(NC4CCCC4)ncnc32)[C@@H]2OC(C)(C)O[C@@H]21
[9-((1R,2R,4R,5R)-4-ethynyl-7,7-dimethyl-3,6,8-trioxabicyclo[3.3.0]oct-2-yl)purin-6-yl]cyclopentylamine
C#C[C@H]1O[C@@H](n2cnc3c(NC4CCCC4)ncnc32)[C@H](O)[C@@H]1O
(4S,2R,3R,5R)-2-[6-(cyclopentylamino)purin-9-yl]-5-ethynyloxolane-3,4-diol

反应条件

温度
75°CELSIUS
详细条件
See reaction.notes.procedure_details.

后处理

  1. 1
    其他Solvent was removed under reduced pressure
  2. 2
    其他the residue purified by preparative TLC
  3. 3
    洗涤eluting with methanol:methylene chloride (1:8)

实验过程

A solution of [9-((1R,2R,4R,5R)-4-ethynyl-7,7-dimethyl-3,6,8-trioxabicyclo[3.3.0]oct-2-yl)purin-6-yl]cyclopentylamine (0.28 g) was dissolved in 20 ml of a mixture of acetic acid:water (80:20) and stirred overnight at 75° C. Solvent was removed under reduced pressure, and the residue purified by preparative TLC, eluting with methanol:methylene chloride (1:8), to yield (4S,2R,3R,5R)-2-[6-(cyclopentylamino)purin-9-yl]-5-ethynyloxolane-3,4-diol, a compound of Formula I.

来源

DOI: 10.6084/m9.figshare.5104873.v1专利: US07022681B2uspto-grants-2006_04