CAS: 876-08-4; 4-(Chloromethyl)Benzoyl Chloride

上下游产品

para-chlorotoluene p-(chloromethyl)benzoic acid 4-methyl-benzoyl chloride 4-bromomethylbenzoic Acid ethyl 4-chloromethylbenzoate p-acetoxymethyl benzoic acid p-(chloromethyl)benzoic acid p-methyloxycarbonylbenzyl chloride

4-羟甲基苯甲酸置于氯化亚砜体系中,用 氯仿 作为反应溶剂,化学反应 5.0H,反应生成 4-氯甲基苯甲酰氯
参考文献:含有 2,6-取代嘌呤作为潜在蛋白激酶抑制剂的新型 4-甲基苯甲酰胺衍生物的合成,体外和硅胶抗癌活性
标题:含有 2,6-取代嘌呤作为潜在蛋白激酶抑制剂的新型 4-甲基苯甲酰胺衍生物的合成,体外和硅胶抗癌活性
摘要:一类新的潜在的蛋白激酶抑制剂的7-16以高产率使用各种取代的嘌呤的合成.最有希望的化合物7和10对七种癌细胞系表现出抑制活性.化合物7和10的 Ic 50值对于k562 细胞分别为 2.27 和 2.53 μm,对于 Hl-60 细胞为 1.42 和 1.52 μm,对于 Okp-Gs 细胞分别为 4.56 和 24.77 μm.此外,化合物7和10剂量依赖性地诱导细胞凋亡和细胞周期停滞在 G2/m 期,阻止 Okp-Gs 细胞的细胞分裂.化合物7,9,和10在 1 μm 的浓度下对 Pdgfrα 和 Pdgfrβ 显示出 36-45% 的抑制活性.分子建模实验表明,获得的化合物可以作为 1 型(化合物7,Atp 竞争性)或 2 型(化合物10,变构)抑制剂与 Pdgfrα 结合,具体取决于分子酰胺部分中的取代基.
DOI:10.3390/ijms222312738

专利信息

专利号:US-2009306400-A1
优先权日:2006-03-27
标 题:Convergent process for the synthesis of taxane derivatives.
发明人：HENRI JOHN T; MCCHESNEY JAMES D; VENKATARAMAN SYLESH K; LAMB RODGER L; FOSTER JONATHAN E; SUMNER CHRISTIAN M; YE SHANGPING
权利人:HENRI JOHN T; MCCHESNEY JAMES D; VENKATARAMAN SYLESH K; LAMB RODGER L; FOSTER JONATHAN E; SUMNER CHRISTIAN M; YE SHANGPING
摘要:The present invention is broadly directed to novel compounds useful for the synthesis of biologically active compounds, including taxane derivatives, and convergent processes for the preparation of these taxane derivatives and their intermediates.

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:WO-2013035102-A1
优先权日:2011-09-05
标 题 :Processes for the preparation of imatinib base and intermediates thereof
发明人：KOMPELLA AMALA KISHAN; RACHAKONDA SREENIVAS; GAMPA VENU GOPALA KRISHNA; ADIBHATLA KALI SATYA BHUJANGA RAO; NANNAPANENI VENKAIAH CHOWDARY
权利人:NATCO PHARMA LTD; KOMPELLA AMALA KISHAN; RACHAKONDA SREENIVAS; GAMPA VENU GOPALA KRISHNA; ADIBHATLA KALI SATYA BHUJANGA RAO; NANNAPANENI VENKAIAH CHOWDARY
摘要:The invention relates to an improved process for the preparation of highly pure imatinib base (99.99% HPLC purity) of formula (I) and the pharmaceutically acceptable acid addition salts thereof. This invention also relates to processes for the preparation of the intermediates in the synthesis of imatinib base.