合成目标产物 3-(Chloromethyl)Benzoyl Chloride 主要起始原料 Formaldehyde And Benzotrichloride
(文献来源)合成步骤主要原料 Formaldehyde 和 Benzotrichloride
📜3-溴甲基苯甲酸置于氯化亚砜体系中,用99.9%的收率获得产物3-(氯甲基)苯甲酰氯 参考文献: Novel Compounds As Histone Deacetylase 6 Inhibitors And Pharmaceutical Compositions Comprising The Same[fr] Nouveaux Composés En Tant Qu'Inhibiteurs De L'Histone Désacétylase 6 Et Compositions Pharmaceutiques Les Comprenant 标题: Novel Compounds As Histone Deacetylase 6 Inhibitors And Pharmaceutical Compositions Comprising The Same[fr] Nouveaux Composés En Tant Qu'Inhibiteurs De L'Histone Désacétylase 6 Et Compositions Pharmaceutiques Les Comprenant 摘要:本发明涉及具有组蛋白去乙酰化酶6(hdac6)抑制活性的新化合物,其异构体或其药用盐,其用于制备治疗药物的用途,包括相同的药物组成部分的药物组合物,使用该组合物治疗疾病的方法,以及制备新化合物的方法.根据本发明的新化合物具有组蛋白去乙酰化酶6(hdac6)抑制活性,并且对于预防或治疗hdac6相关疾病(包括癌症,炎症性疾病,自身免疫疾病,神经系统疾病和神经退行性疾病)有效.
专利号:US-5712367-A 优先权日:1989-10-02 标 题:Process for the solubilization of peptides and process for peptide synthesis 发明人:BERNARD JEAN-MARIE; BOUZID KAMEL; GERVAIS CHRISTIAN 权利人:RHONE POULENC CHIMIE 摘要:A process is disclosed for making peptides soluble in a water-immiscible organic solvent, comprising linking a lipophilic group with an amide or ester bond to the terminal carboxyl group of said peptide; when the lipophilic group is linked to L-serine, a molecule is obtained with a solubility in water at 25 DEG C. of less than 30 g/liter. This lipophilic group is non-polymeric and chemically defined. A process is also disclosed for the synthesis of peptides, optionally protected, in a liquid medium, wherein the starting material is an amino acid or peptide made soluble in an organic medium by a lipophilic group A-L linked to the carboxyl function of the starting amino acid or peptide, and are added to amino acids or peptides to be condensed which are activated on their acid function and protected on their amine function and are optionally protected on their side chain. The peptides resulting from the synthesis are used, where appropriate, for the synthesis of medicinal products, vaccines or agri-foodstuff or plant-protection.
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
参考标题:New Heteroditopic, Linked Macrocyclic Systems Derived From Selectively Protected N2S2-, N3O2- And N4-Donor Macrocycles 作者:Jy D. Chartres,Andrew M. Groth,Leonard F. Lindoy,Mark P. Lowe,George V. Meehan 摘要:The Use Of Selectively Tert-Butoxycarbonyl Protected Derivatives Of 1,9-Dithia-5,13-Diazacyclohexadecane 1, 1,7-Dithia-4,11-Diazacyclotetradecane 2, 1,4,8,11-Tetraazacyclotetradecane 3 And 2,5-Dioxa-8,11,14-Triaza-1,6(1,2)-Dibenzenacyclopentadecaphane 4 Has Enabled The Efficient Synthesis Of New Linked Heteroditopic Macrocyclic Systems Incorporating Combinations Of N2S2- And N4- Or N3O2-Donor Sites. Incorporation Of Two Types Of Binding Sites In The Respective Products Makes Them Suitable Candidates For The Synthesis Of A Range Of Mixed-Metal, Di- And Oligo-Nuclear Metal Complexes.
合成参考文献
摘要:Sellars, J. D., Science of Synthesis Knowledge Updates, (2014) 1, 420.