CAS: 603-62-3; 3-Nitrophthalimide

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CAS号641-70-3 3-硝基邻苯二甲酸酐 | CAS号603-11-2 3-硝基邻苯二甲酸 | CAS号24564-71-4 1,2-BENZENEDICA... | CAS号51762-67-5 3-硝基邻苯二甲腈 | CAS号65911-46-8 2-氨甲酰基-6-硝基苯甲酸 | CAS号21606-04-2 2-(甲氧羰基)-6-硝基苯甲酸 | CAS号96385-50-1 3-硝基邻苯二甲二酰胺 | CAS号77326-45-5 2-氨基甲酰基-3-硝基苯甲酸 | CAS号7664-41-7 氨 | CAS号723332-77-2 2-amino-4-nitro... | CAS号606-18-8 2-氨基-3-硝基苯甲酸 | CAS号50573-74-5 2-氨基-6-硝基苯甲酸 | CAS号3682-15-3 3-硝基邻苯二甲酰肼 | CAS号723332-77-2 2-amino-4-nitro... | CAS号190910-88-4 4-硝基-N-碳乙氧基邻苯二甲酰亚胺 | CAS号2593-81-9 1H-Isoindole-1,... | CAS号96385-50-1 3-硝基邻苯二甲二酰胺 | CAS号2257-85-4 N-甲基-4-氨基邻苯二甲酰亚胺 | CAS号2778-84-9 N-乙基-3-硝基酞酰亚氨 | CAS号77326-45-5 2-氨基甲酰基-3-硝基苯甲酸

3-硝基邻苯二甲酸酐置于ammonium Hydroxide体系中,化学反应 2.0H,以93%的收率获得产物3-硝基邻苯二甲酰亚胺
参考文献:Chemoenzymatic Synthesis Of Apremilast: A Study Using Ketoreductases And Lipases
标题:Chemoenzymatic Synthesis Of Apremilast: A Study Using Ketoreductases And Lipases
摘要:在阿普雷米拉斯的化学酶合成中的关键步骤是产生手性醇(R)-1-(3-乙氧基-4-甲氧基苯基)-2-(甲磺基)乙醇,(R)-3.评估了两种酶法来获得(R)-3,一种使用酮还原酶,另一种使用脂肪酶.使用酮还原酶kred-P2-D12对1-(3-乙氧基-4-甲氧基苯基)-2-(甲磺基)乙酮(2)进行生物还原,导致(R)-3,转化率为48%,对映体过量为93% (Ee).通过利用黑曲霉脂肪酶催化,对手性纯(R)-3和4-乙酰氨基异吲哚-1,3-二酮(8)之间的反应,得到了65%的产率和67%的ee的阿普雷米拉斯.
DOI:10.21577/0103-5053.20210012

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:WO-2011098386-A1
优先权日:2010-02-09
标 题 :Process for the preparation of an anthranilic acid derivative
发明人：MURUDI VIKRANT; SHYADLIGERI ASHOK SHANKARAPPA; MISHRA BRIJNANDAN PREMNATH; LUGINBUEHL MARKUS ADOLF; FUERST MAREN
权利人:SYNGENTA PARTICIPATIONS AG; MURUDI VIKRANT; SHYADLIGERI ASHOK SHANKARAPPA; MISHRA BRIJNANDAN PREMNATH; LUGINBUEHL MARKUS ADOLF; FUERST MAREN
摘要:The present invention relates to a novel a process for the preparation of a compound of formula (I) which process comprises adding 1 to 2 mol of sodium hypochlorite with a concentration of 8% to 15% by weight to a suspension of the compound of formula (II) in aqueous sodium hydroxide at a temperature of 5 to 60°C, wherein the concentration of sodium hydroxide in the suspension is from 5 to 25 % by weight; and acidifying the reaction mass with concentrated hydrochloric acid to a pH of 1.5 to 2.0 and wherein said process is carried out as a one-pot synthesis without isolation of intermediates.