专利号:WO-2016005407-A1 优先权日:2014-07-07 标 题:One-pot synthesis of squaramides 发明人:MÃ?RQUEZ LÓPEZ MARÃ?A EUGENIA; ALEGRE REQUENA JUAN VICENTE; PÉREZ HERRERA RAQUEL 权利人:UNIV ZARAGOZA; CONSEJO SUPERIOR INVESTIGACION 摘要:The present invention refers to the first one-pot synthesis of squaramides. The one-pot synthesis of squaramides described herein is an easy and straightforward procedure to obtain squaramide derivatives which saves energy, avoids time consuming purification steps, reduces costs and provides better yields as compared with those squaramides obtained through the traditional 'stop-and-go' approach. Moreover, the authors of the present invention herein demonstrate the efficiency of this one-pot process with the synthesis of three biologically active structures, improving in most of the cases the results of the previous stepwise syntheses.
专利号:US-8476441-B2 优先权日:2009-01-29 标 题 :Intermediates in the enantioselective synthesis of 3-(aminomethyl)-5-methyl-hexanoic acid 发明人:CONNON STEPHEN JOSEPH; PESCHIULLI ALDO; MARKEY LYN 权利人:CONNON STEPHEN JOSEPH; PESCHIULLI ALDO; MARKEY LYN; TRINITY COLLEGE DUBLIN 摘要:(S)-(+)-3-(aminomethyl)-5-methyl-hexanoic acid or (S)-pregabalin is an anticonvulsive drug. In addition to its use as an anticonvulsive agent, pregabalin has also been indicated as a medicament in the treatment of anxiety, neuropathic pain and pain in patients with fibromyalgia. Provided herein are thioester intermediates in the synthesis of and processes for the synthesis of 3-(aminomethyl)-5-methyl-hexanoic acid in the (R) or (S) configuration.
专利号:US-2003162992-A1 优先权日:2001-12-14 标 题 :Preparation of intermediates useful in the synthesis of antiviral nucleosides 发明人:WATANABE KYOICHI A; DU JINFA 摘要:The present invention is an efficient process for the manufacture of α-acyloxyacetaldehyde, a key intermediate in the synthesis of 1,3-oxathiolane and 1,3-dioxolane nucleosides.
专利号:US-6133409-A 优先权日:1996-12-19 标 题:Process for the solid phase synthesis of aldehyde, ketone, oxime, amine, hydroxamic acid and αβ-unsaturated carboxylic acid and aldehyde compounds 发明人:SALVINO JOSEPH M; MORTON GEORGE C; MASON HELEN J; LABAUDINIERE RICHARD F 权利人:AVENTIS PHARM PROD INC 摘要:This invention is directed to a process for the solid phase synthesis of aldehyde, ketone, oxime, amine, hydroxamic acid and alpha , beta -unsaturated carboxylic acid and aldehyde compounds and to polymeric hydroxylamine resin compounds useful therefor.
专利号:US-6710208-B2 优先权日:1996-12-19 标题 :Process for the solid phase synthesis of aldehyde, ketone, oxime, amine, hydroxamic acid and α,β-unsaturated carboxylic acid and aldehyde compounds 发明人:SALVINO JOSEPH M; MORTON GEORGE C; MASON HELEN J; LABAUDINIERE RICHARD F 权利人:AVENTIS PHARMA INC 摘要:This invention is directed to a process for the solid phase synthesis of aldehyde, ketone, oxime, amine, hydroxamic acid and α,β-unsaturated carboxylic acid and aldehyde compounds and to polymeric hydroxylamine resin compounds useful therefor.
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.
参考标题:Silver-Catalyzed Oxidative Activation Of Benzylic Ch Bonds For The Synthesis Of Difluoromethylated Arenes 作者:Peng Xu,Shuo Guo,Liyan Wang,Pingping Tang |发布日期:2014.6.2 摘要:A Mild And Catalytic Method To Form Difluoromethylated Arenes Through The Activation Of Benzylic Ch Bonds Has Been Developed. Utilizing Agno3 As The Catalyst, Various Arenes With Diverse Functional Groups Undergo Activation/fluorination Of Benzylic Ch Bonds With Commercially Available Selectfluor Reagent As A Source Of Fluorine In Aqueous Solution. The Reaction Is Operationally Simple And Amenable
合成参考文献
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