反应 #2171069

ord-052283e0dbbf46519d76d1698da6914b

反应方程式

Nc1ncnc2c1ncn2CCOCP(=O)(O)O
adefovir
CCCCCCCCCCCCCCCCOCCCO
3-hexadecyloxy-1-propanol
C(=NC1CCCCC1)=NC1CCCCC1
DCC
CCCCCCCCCCCCCCCCOCCCOP(=O)(O)COCCn1cnc2c(N)ncnc21
hexadecyloxypropyl-adefovir

溶剂

反应条件

详细条件
See reaction.notes.procedure_details.

后处理

  1. 1
    温度The mixture was heated
  2. 2
    温度to reflux
  3. 3
    温度then cooled
  4. 4
    过滤filtered
  5. 5
    浓缩The filtrate was concentrated under reduced pressure
  6. 6
    洗涤Elution of the column with 9:1 dichloromethane/methanol

实验过程

To a mixture of adefovir (1.36 g, 5 mmol) and 3-hexadecyloxy-1-propanol (1.8 g, 6 mmol) in dry pyridine was added DCC (2.06 g, 10 mmol). The mixture was heated to reflux and stirred 18 h then cooled and filtered. The filtrate was concentrated under reduced pressure and the residue was applied to a short column of silica gel. Elution of the column with 9:1 dichloromethane/methanol yielded hexadecyloxypropyl-adefovir (HDP-ADV) as a white powder.

来源

DOI: 10.6084/m9.figshare.5104873.v1专利: US06716825B2uspto-grants-2004_04