📜对甲氧基苯磺酰氯,3-丁炔-1-醇置于吡啶体系中,用 二氯甲烷 用作溶剂,以93%的收率获得对甲苯磺酸 3-丁炔酯 参考文献:Evaluation And Optimization Of Antifibrotic Activity Of Cinnamoyl Anthranilates 标题:Evaluation And Optimization Of Antifibrotic Activity Of Cinnamoyl Anthranilates 摘要:Tranilast Is An Anti-Inflammatory Drug In Use For Asthma And Atopic Dermatitis. In Studies Over The Last Decade It Has Been Revealed That Tranilast Can Reduce Fibrosis occurring In The Kidney During Diabetes,Thereby Delaying And/or Preventing Kidney Dysfunction. We Report A Structure-Activity Study Aimed At Optimizing The Antifibrotic Activity Of Tranilast. A Series Of Cinnamoyl Anthranilates Were Prepared And Assessed For Their Ability To Prevent Tgf-Beta-Stimulated Production Of Collagen In Cultured Renal Mesangial Cells. We Reveal Derivatives With Improved Potency And Reduced Cellular Toxicity Relative To Tranilast. 3-Methoxy-4-Propargyloxycinnamoyl Anthranilate Reduces Albuminuria In A Rat Model Of Progressive Diabetes,And Thus Has Potential As An Innovative Treatment For Diabetic Nephropathy. (C) 2009 Elsevier Ltd. All Rights Reserved. Doi:10.1016/j.Bmcl.2009.09.120
专利号:US-2025026768-A1 优先权日:2023-06-30 标题:Method for the synthesis of axially chiral organoboron compounds 发明人:PING YIFAN; CHE CHI-MING 权利人:LABORATORY FOR SYNTHETIC CHEMISTRY AND CHEMICAL BIOLOGY LTD 摘要:A highly efficient and atroposelective Rh-catalyzed [2+2+2] cycloaddition for the synthesis of axially chiral aryboron compounds is developed. The reactions of diynes and alkynylborons smoothly occur in an atom-economical manner, affording a variety of C—B atropisomers in excellent yields and enantioselectivities. The protocol features mild conditions, broad substrate scope, and good functional tolerance. The obtained C—B atropisomers show powerful synthetic applications in terms of producing novel chiral phosphine ligands.
专利号:US-7402703-B2 优先权日:2005-06-08 标 题:Stereoselective synthesis of (E)-vinylboronic esters via a Zr mediated hydroboration of alkynes 发明人:WANG YANONG DANIEL 权利人:WYETH CORP 摘要:There is herein provided a process for Zr-mediated hydroboration of alkynes which offers (E)-vinylboronic esters in high yield with stereoselectivity and regioselectivity.
专利号:US-2006281943-A1 优先权日:2005-06-08 标题 :Stereoselective synthesis of (E)-vinylboronic esters via a Zr mediated hydroboration of alkynes
专利号:RU-2071962-C1 优先权日:1987-12-18 标题 :Method of synthesis of triazolo-[4,3-a]-[1,4]-diazepines
专利号:WO-2006132896-A2 优先权日:2005-06-08 标题:Stereoselective synthesis of (e)-vinylboronic esters via a zr mediated hydroboration of alkynes
专利号:US-8093229-B2 优先权日:2005-03-30 标题 :Alkynyl pyrrolo[2,3-d]pyrimidines and related analogs as HSP90-inhibitors 发明人:KASIBHATLA SRINIVAS RAO; BIAMONTE MARCO ANTONIO; SHI JIANDONG; BOEHM MARCUS F 权利人:KASIBHATLA SRINIVAS RAO; BIAMONTE MARCO ANTONIO; SHI JIANDONG; BOEHM MARCUS F; CONFORMA THERAPEUTICS CORP 摘要:Alkynyl pyrrolo [2,3-d] pyrimidines of Formula I are described and demonstrated to have utility as Heat Shock Protein 90 (HSP90) inhibiting agents used in the treatment and prevention of various HSP90 mediated disorders. Methods of synthesis and use of such compounds are also described and claimed.
[参考文献]: Beck A, Et Al. Strategies And Challenges For The Next Generation Of Antibody-Drug Conjugates. Nat Rev Drug Discov. 2017 May;16(5):315-337. [参考文献]: S A Glase, Et Al. Aryl 1-But-3-Ynyl-4-Phenyl-1,2,3,6-Tetrahydropyridines As Potential Antipsychotic Agents: Synthesis And Structure-Activity Relationships. J Med Chem. 1996 Aug 2;39(16):3179-87. [参考文献]: Sean C Turner, Et Al. A New Class Of Histamine H(3)-Receptor Antagonists: Synthesis And Structure-Activity Relationships Of 7,8,9,10-Tetrahydro-6H-Cyclohepta[b]Quinolines. Bioorg Med Chem Lett. 2003 Jul 7;13(13):2131-5.
合成参考文献
摘要:Diver, S. T., Science of Synthesis, (2009) 46, 130. 摘要:Michalak, M.; Gulajski, L.; Grela, K., Science of Synthesis, (2010) 47, 392. 摘要:Aguilar, E.; López, L. A., Science of Synthesis Knowledge Updates, (2014) 2, 60. 摘要:Santi, C., Science of Synthesis Knowledge Updates, (2013) 2, 416. 摘要:Calleja, P.; Dorel, R.; Echavarren, A. M., Science of Synthesis: Catalytic Oxidation in Organic Synthesis, (2017) 1, 480.