专利号:US-7189864-B2 优先权日:1990-11-19 标 题:Method of preparing 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 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 diastereoselective epoxide from a chiral alpha amino aldehyde.
专利号:US-6022996-A 优先权日:1990-11-19 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 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 diastereoselective epoxide from a chiral alpha amino aldehyde.
专利号:EP-0641333-B1 优先权日:1992-05-20 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 权利人:SEARLE & CO; MONSANTO 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 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.
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-2002161234-A1 优先权日:1990-11-19 标 题 :Method of preparing intermediates useful in synthesis of retroviral protease inhibitors
专利号:US-5872299-A 优先权日:1990-11-19 标 题 :Method of preparing intermediates for 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 diastereoselective epoxide or cyanohydrin from a chiral alpha amino aldehyde.
参考标题:Relay Catalysis: Enantioselective Synthesis Of Cyclic Benzo-Fused Homoallylic Alcohols By Chiral Brønsted Acid-Catalyzed Allylboration/ring Closing Metathesis 作者:Santos Fustero,Elsa Rodríguez,Rubén Lázaro,Lidia Herrera,Silvia Catalán,Pablo Barrio |发布日期:2013.4.15 摘要:Six‐ And Seven‐membered Benzo‐fused Cyclic Homoallylic Alcohols Can Be Readily Synthesized By A Tandem Chiral Brønsted Acid‐catalyzed Allyl (Crotyl)Boration/ring Closing Metathesis Sequence Performed Under Orthogonal Relay Catalysis Conditions. Excellent Enantio‐ And Diastereoselectivities Are Obtained In Most Of The Cases. In Addition, The Parent Crotylboration/rcm Process Is Also Described. The Required
合成参考文献
参考文献:10.1055/s-0036-1588734 摘要:Dodonova J, Tumkevicius S. Fused Pyrrolo[2,3-d]pyrimidines (7-Deazapurines) by Palladium-Catalyzed Direct N–H and C–H Arylation Reactions. Synthesis. 2017 Mar 02;49(11):2523–34. doi: 10.1055/s-0036-1588734.