发明名称 IMPROVED PRODUCTION OF 2',2'-DIFLUORONUCLEOSIDES
摘要 <p>PROBLEM TO BE SOLVED: To efficiently produce the subject compounds, having a specificα/β- anomeric ratio and useful as an antiviral agent, etc., by reacting a protected specific carbohydrate with a suitable base, then reacting the resultant compound with a strong base and removing benzoyl protecting groups. SOLUTION: A protected carbohydrate represented by formula I (L is an eliminable group) is reacted with a suitable base represented by the formula BH B is a group represented by formula II [X is N or a group represented by C-R<4> (R<4> is H, a 1-4C alkyl, amino or a halogen) ; R" is H, a l-4C alkyl, etc.], a group represented by formula III, etc.} to provide a compound represented by formula IV (Rs are each benzoyl), which, as desired, is reacted with a strong base or a moderately strong base to eliminate benzoyl protecting groups. Thereby, a compound represented by formula IV (Rs are each H) is produced to thereby afford the objective 2'-deoxy-2',2'-difluoronucleoside represented by formula IV (Rs are each H or benzoyl) at about 1:1α/β-anomeric ratio.</p>
申请公布号 JPH1072484(A) 申请公布日期 1998.03.17
申请号 JP19970227948 申请日期 1997.08.25
申请人 ELI LILLY & CO 发明人 CHOU TA-SEN;HEATH PERRY C;PATTERSON LAWRENCE E
分类号 C07H1/06;A61K31/365;A61K31/70;A61K31/7024;A61K31/7042;A61K31/7052;A61K31/7056;A61K31/706;A61K31/7064;A61K31/7068;A61K31/7072;A61K31/7076;A61K31/708;A61P35/00;C07D307/32;C07D307/33;C07H7/02;C07H13/08;C07H19/056;C07H19/06;C07H19/067;C07H19/12;C07H19/16;C07H19/167;(IPC1-7):C07H19/12 主分类号 C07H1/06
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