发明名称 |
METHOD FOR MAKING INTERMEDIATES USEFUL IN SYNTHESIS OF RETROVIRAL PROTEASE INHIBITORS. |
摘要 |
<p>A synthesis is described for intermediates which are readily amenable to the large scale preparation of hydroxyethylurea-based chiral HIV protease inhibitors. The method includes forming a diastereoselective epoxide compound of formula (I) from a chiral alpha amino aldehyde and halomethyllithium as an organometallic methylene-adding reagent. In formula (I) R<1> is selected from alkyl, aryl, cycloalkyl, cycloalkylalkyl and arylalkyl, which are optionally substituted with a group selected from alkyl, halogen, NO2, OR<9> or SR<9>, where R<9> represents hydrogen or alkyl; and P<1> and P<2> independently are selected from amine protecting groups, including but not limited to, arylalkyl, substituted arylalkyl, cycloalkenylalkyl and substituted cycloalkenylalkyl, allyl, substituted allyl, acyl, alkoxycarbonyl, aralkoxycarbonyl and silyl.</p> |
申请公布号 |
GR3020814(T3) |
申请公布日期 |
1996.11.30 |
申请号 |
GR19960402048T |
申请日期 |
1996.08.16 |
申请人 |
G.D. SEARLE & CO.;MONSANTO COMPANY |
发明人 |
NG, JOHN, S.;PRZYBYLA, CLAIRE, A.;MUELLER, RICHARD, A.;VAZQUEZ, MICHAEL, L.;GETMAN, DANIEL, P. |
分类号 |
C07D301/02;C07B53/00;C07C209/68;C07C211/27;C07C213/00;C07C213/02;C07C213/08;C07C215/28;C07C223/02;C07C233/31;C07C271/16;C07C275/22;C07C275/24;C07C317/44;C07C323/63;C07D215/48;C07D301/06;C07D303/36;C07F7/18;C07K5/02;(IPC1-7):C07D303/36 |
主分类号 |
C07D301/02 |
代理机构 |
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代理人 |
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主权项 |
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地址 |
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