发明授权
US4775759A Synthesis and utilization of 17-methyl and
17-cyclopropylmethyl-3,14-dihydroxy-4,5.alpha.-epoxy
6.beta.-fluoromorphinans (foxy and cyclofoxy) as (18F)-labeled opioid
ligands for position emission transaxial tomography (PETT)
失效
合成和利用17位甲基和17-环丙基甲基-3,14-二羟基-4,5α-环氧6β-氟吗啡喃（Foxy和环氧基）作为（18F）标记的阿片样物质配体用于位置发射横断层扫描（PETT）
- 专利标题： Synthesis and utilization of 17-methyl and 17-cyclopropylmethyl-3,14-dihydroxy-4,5.alpha.-epoxy 6.beta.-fluoromorphinans (foxy and cyclofoxy) as (18F)-labeled opioid ligands for position emission transaxial tomography (PETT)
- 专利标题（中）： 合成和利用17位甲基和17-环丙基甲基-3,14-二羟基-4,5α-环氧6β-氟吗啡喃（Foxy和环氧基）作为（18F）标记的阿片样物质配体用于位置发射横断层扫描（PETT）
-
申请号： US675276申请日： 1984-11-27
-
公开(公告)号： US4775759A公开(公告)日： 1988-10-04
- 发明人: Kenner C. Rice , Candace B. Pert , Terrence R. Burke, Jr. , Steven M. Larson , William C. Eckelman , Michael A. Channing
- 申请人： Kenner C. Rice , Candace B. Pert , Terrence R. Burke, Jr. , Steven M. Larson , William C. Eckelman , Michael A. Channing
- 申请人地址： DC Washington
- 专利权人： The United States of America as represented by the Department of Health and Human Services
- 当前专利权人： The United States of America as represented by the Department of Health and Human Services
- 当前专利权人地址： DC Washington
- 主分类号： A61K51/04
- IPC分类号： A61K51/04 ; C07D489/08 ; A61K43/00 ; A61K49/02
摘要：
Fluorinated derivatives 3,14-dihydroxy-4,5.alpha.-epoxy-6.beta.-fluoro-17-methylmorphinan ("fluorooxymorphone"; FOXY, compound 10) and 17-cyclopropylmethyl-3,14-dihydroxy-4,5.alpha.-epoxy-6.beta.-fluoromorphinan (CYCLOFOXY, compound 18) are prepared based upon the structures of the potent opioid agonist oxymorphone 4 and the antagonist naltrexone 11, respectively. Fluorine was introduced in the final stages of synthesis by a facile nucleophilic displacement with fluoride ion of the 6.alpha.-triflate functions in 8 and 16. The synthetic procedures were suitable for the production of the corresponding positron emitting .sup.18 F-labeled analogs .sup.18 F-FOXY and .sup.18 F-CYCLOFOXY, which are useful for in vivo studies of the opioid receptor system using positron emission transaxial tomography. In addition, the tritiation of FOXY (10) to high specific activity is noted.
公开/授权文献
- US5743525A Sporting event wagering system 公开/授权日：1998-04-28
信息查询
