CAS: 55117-15-2; 1-Chloro-2-(Chloromethyl)-3-Fluorobenzene

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CAS号443-83-4 2-氯-6-氟甲苯 | CAS号56456-50-9 2-氯-6-氟苄醇 | CAS号68220-23-5 3-[(2-chloro-6-... | CAS号55779-18-5 阿普西特 | CAS号196862-01-8 1-chloro-2-ethe... | CAS号190521-88-1 diethyl 2-(2-ch... | CAS号2829-57-4 [1,2,5]thiadiaz... | CAS号64825-52-1 (2-chloro-6-flu... | CAS号15205-15-9 2-氯-6-氟苄胺 | CAS号70091-21-3 9-(2-chloro-6-f... | CAS号70091-23-5 9-(2-chloro-6-f...

2-氯-6-氟苄醇置于吡啶,氯化亚砜体系中,用 二氯甲烷 作为反应溶剂,以90 %的收率获得产物2-氯-6-氟氯苄
参考文献:2,6-二卤代二苯乙烯衍生物的设计与合成作为潜在的抗炎和抗肿瘤药物
标题:2,6-二卤代二苯乙烯衍生物的设计与合成作为潜在的抗炎和抗肿瘤药物
摘要:在本研究中,设计,合成并测定了三个系列的 2,6-二卤代茋衍生物的抗炎和细胞毒活性.所有 62 种化合物在体内斑马鱼模型中均显示出潜在的抗炎活性,卤素和吡啶的加入导致显着改善效果.其中,取代吡啶的dhs2U和dhs3U在20 μm时表现出比阳性药物吲哚美辛更高的抑制率,分别为94.59%和90.54%.此外,带有 2,5-二甲氧基的dhs3G对 K562 细胞表现出强大的细胞毒活性,Ic 为50值 3.12 μm 以及对正常细胞活力的适当选择性.这些结果表明,2,6-二卤代二苯乙烯可以作为进一步开发抗炎和抗肿瘤药物的非常好起点.
DOI:10.1016/j.Fitote.2023.105493

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-8034966-B1
优先权日:2008-02-20
标 题:Phenoxyisobutyric acid compounds and methods for synthesis
发明人：LALEZARI IRAJ; FABRICANT JILL
权利人:CELL VIABLE CORP
摘要:The present invention provides a process for the synthesis of substituted arylureidophenoxymethylpropionic acid and related compounds including bifunctional and tetrafunctional derivatives. The compounds are useful for inhibiting the formation of AGEs (Aminaglycation end products).

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