- 专利标题： Synthesis of 2′-fluoro-6′-methylene-carbocyclic adenosine (FMCA) and 2′-fluoro-6′-methylene-carbocyclic guanosine (FMCG)
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申请号： US16083128申请日： 2017-03-01
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公开(公告)号： US10533008B2公开(公告)日： 2020-01-14
- 发明人: Chung K. Chu , Varughese Alexander Mulamootttil , Ram C. Mishra , Uma Sharan Singh
- 申请人： UNIVERSITY OF GEORGIA RESEARCH FOUNDATION, IONC.
- 申请人地址： US GA Atlanta
- 专利权人： UNIVERSITY OF GEORGIA RESEARCH FOUNDATION, INC.
- 当前专利权人： UNIVERSITY OF GEORGIA RESEARCH FOUNDATION, INC.
- 当前专利权人地址： US GA Atlanta
- 代理商 Henry D. Coleman; R. Neil Sudol
- 国际申请： PCT/US2017/020165 WO 20170301
- 国际公布： WO2017/176392 WO 20171012
- 主分类号： C07D473/34
- IPC分类号： C07D473/34 ; C07D317/44 ; C07C41/26 ; C07C41/30 ; C07D473/18 ; C07D473/26 ; C07D473/40 ; C07F9/6561 ; C07C41/28 ; A61P31/20 ; C07C43/196
摘要：
The invention provides a new convergent approach for the synthesis of 2′-fluoro-6′-methylene-carbocyclic adenosine (FMCA) and 2′-fluoro-6′-methylene-carbocyclic guanosine (FMCG) from a readily available starting material in eight steps. An efficient and practical methodology for stereospecific preparation of a versatile carbocyclic key intermediate, (1S,3R,4R)-3-tert-butoxy-4-(tert-butoxymethyl)-2-fluoro-5-methylenecyclopentanol (compound 8 of scheme 1A or a) in only six (6) steps is also provided. Prodrugs of these compounds are also prepared.
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