专利号:US-6281367-B1 优先权日:1998-03-20 标 题:Process for the synthesis of HIV protease inhibitors 发明人:AL-FARHAN EMILE; DEININGER DAVID D; MCGHIE STEPHEN; O'CALLAGHAN JOHN; ROBERTSON MARK STUART; RODGERS KEITH; ROUT STEPHEN JOHN; SINGH HARDEW; TUNG ROGER DENNIS 权利人:GLAXO WELLCOME INC 摘要:An improved process for the synthesis of (3S)-tetrahydro-3-furyl N-[(1S,2R)-3 -(4-amino-N-isobutylbenzenesulphonamido)-1-benzyl-2-hydroxypropyl]carbamate comprising four steps form the compound of formula A and a novel intermediate thereto.
专利号:EP-0855388-B1 优先权日:1993-11-23 标 题 :Method for making intermediates useful in synthesis of retroviral protease inhibitors 发明人:NG JOHN S; PRZYBYLA CLAIRE A; MUELLER RICHARD A; VAZQUEZ MICHAEL L; GETMAN DANIEL P; FRESKOS JOHN J; DECRESCENZO GARY A; BERTENSHAW DEBORAH E; HEINTZ ROBERT M; ZHANG SUHONG; LIU CHIN; LANEMAN SCOTT A 权利人:SEARLE & CO 摘要: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 cyanohydrin from a chiral alpha amino aldehyde.
专利号:US-6140505-A 优先权日:1995-03-10 标 题:Synthesis of benzo fused heterocyclic sulfonyl chlorides
专利号:US-5648511-A 优先权日:1990-11-19 标题 :Method for making intermediates useful in the synthesis of retroviral protease inhibitors
专利号:US-6127556-A 优先权日:1996-12-31 标 题 :Epoxide formation by continuous in-situ synthesis process 发明人:LIU CHIN; NG JOHN S; BEHLING JAMES R; CAMPBELL ARTHUR L 权利人:SEARLE & CO 摘要:In a method of preparing an aminoepoxide wherein a protected aminoaldehyde is reacted with a halomethyl organometallic reagent in an appropriate solvent at a temperature above -80° C., wherein said halomethyl organometallic reagent is formed by reaction between an organometallic reagent and a dihalomethane, the improvement comprising flowing said protected aminoaldehyde into a mixing zone maintained at a temperature below 0° C., also flowing said halomethyl organometallic reagent in said mixing zone for contacting in said mixing zone with said protected aminoaldehyde and also withdrawing from said mixing zone reaction products of said protected aminoaldehyde and said halomethyl organometallic reagent.
专利号:EP-1066276-A1 优先权日:1998-03-20 标题 :Process for the synthesis of hiv protease inhibitors