基本信息:
- 专利标题： Process for preparing heterocyclic compounds
- 专利标题（中）：制备杂环化合物的方法
- 申请号：EP86308207 申请日：1986-10-22
- 公开(公告)号：EP0221725A3 公开(公告)日：1988-03-23
- 发明人： Hayman, David Frank , Brodie, Alastair Couper , Procopiou, Panayiotis Alexandrou
- 申请人： GLAXO GROUP LIMITED
- 专利权人： GLAXO GROUP LIMITED
- 当前专利权人： GLAXO GROUP LIMITED
- 优先权： GB8526209 19851023
- 主分类号： C07D319/20
- IPC分类号： C07D319/20 ; C07C43/23 ; C07D491/056 ; C07D319/00 ; C07D209/00
摘要：
A compound of formula (I)
is prepared by cyclising a compound of formula (IIa) or (IIb) or a mixture thereof
wherein
X is hydroxyl or halogen and R' and R 2 independently, represent hydroxy protecting groups) followed by removal of the protecting groups R 1 and R 2 . The compound (I) is of use as an intermediate inthestere- oselective preparation of (±)trans -5-fluoro-2,3,3a,9a-tetra- hydro-1H-[1,4]benzodioxino[2,3-c) pyrrole, which is a selective α 2 -adrenoreceptor antagonist and is thus of potential value, in particular, for the treatment or prevention of depression.
is prepared by cyclising a compound of formula (IIa) or (IIb) or a mixture thereof
wherein
X is hydroxyl or halogen and R' and R 2 independently, represent hydroxy protecting groups) followed by removal of the protecting groups R 1 and R 2 . The compound (I) is of use as an intermediate inthestere- oselective preparation of (±)trans -5-fluoro-2,3,3a,9a-tetra- hydro-1H-[1,4]benzodioxino[2,3-c) pyrrole, which is a selective α 2 -adrenoreceptor antagonist and is thus of potential value, in particular, for the treatment or prevention of depression.
IPC结构图谱:
| C | 化学；冶金 |
| --C07 | 有机化学 |
| ----C07D | 杂环化合物 |
| ------C07D319/00 | 杂环化合物，含六元环，有两个氧原子作为仅有的杂环原子 |
| --------C07D319/04 | .1,3-二烷；氢化1,3-二烷 |
| ----------C07D319/14 | ..和碳环或碳环系稠合 |
| ------------C07D319/16 | ...与1个六元环稠合 |
| --------------C07D319/20 | ....有取代基连在杂环上 |