CAS: 3290-01-5; 1,2-Dichloro-3-(Chloromethyl)Benzene

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CAS号38594-42-2 2,3-二氯苯甲醇 | CAS号608-27-5 2,3-二氯苯胺 | CAS号6334-18-5 2,3-二氯苯甲醛 | CAS号7647-18-9 氯化锑(V) | CAS号100-44-7 氯化苄 | CAS号3218-45-9 2,3-二氯氰苄

2,3-二氯苯甲醛置于sodium Tetrahydroborate,氯化亚砜体系中,用 甲醇,苯 作为反应溶剂,化学反应生成 1,2-二氯-3-(氯甲基)苯
参考文献:Antihypertensive Activity Of 6-Arylpyrido[2,3-D]Pyrimidin-7-Amine Derivatives
标题:Antihypertensive Activity Of 6-Arylpyrido[2,3-D]Pyrimidin-7-Amine Derivatives
摘要:A Series Of 51 6-Arylpyrido[2,3-D]Pyrimidin-7-Amine Derivatives Was Prepared And Evaluated For Antihypertensive Activity In The Conscious Spontaneously Hypertensive Rat. A Number Of These Compounds,Notably 6-(2,6-Dichlorophenyl)-2-Methylpyrido[2,3-D]Pyrimidin-7-Amine (36),Lowered Blood Pressure In These Rats In A Gradual And Sustained Manner To Normotensive Levels At Oral Doses Of 10-50 Mg/kg. Normalized Blood Pressure Levels Could Then Be Maintained By Single Daily Oral Doses. The Effect Of Structural Variation In The 6-Aryl Group And In The 2 And 4 Positions Of The Pyridopyrimidine Ring On Activity Is Reported And Discussed.
DOI:10.1021/jm00136A006

专利信息

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.