CAS: 511-18-2; 24-Nor-5β-Cholanoic Acid

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    上下游产品

    24-Nor-Lithodeoxycholic Acid 4057-91-4
    Methyl-23Nor-5β-Cholonat 6035-23-0
    石胆酸 Lithocholic Acid 434-13-9
    (3R)-3-[(3R,5S,7R,10S,13R,17R)-3,7-二羟基-10,13-二甲基十六碳氢-1H-环戊二烯并[a]菲-17-基]丁酸 Nor-Chenodeoxycholic Acid 86386-61-0
    5β-Cholanoic Acid-(24)-Ethyl Ester 5795-90-4
    26.27-Bis-Nor-5β-Cholestan-24-On 14949-16-7
    3α-Formyloxy-5β-Cholan-24-Oic Acid 5015-59-8

    合成工艺路线路线简述

      📜3α-Formyloxy-5β-Cholan-24-Oic Acid置于吡啶,Palladium Hydroxide,20 Wt% On Carbon,氢气,Lithium Carbonate,对甲苯磺酸,三氟乙酸,三氟乙酸酐,Potassium Hydroxide,Lithium Bromide,Sodium Hydroxide,Sodium Nitrite体系中,用 四氢呋喃,甲醇,水,N,N-二甲基甲酰胺 作为反应溶剂,化学反应 29.0H,反应生成 24-去甲-5Beta-胆烷-23-酸
      参考文献:Investigation On Bile Acid Receptor Regulators. Discovery Of Cholanoic Acid Derivatives With Dual G-Protein Coupled Bile Acid Receptor 1 (Gpbar1) Antagonistic And Farnesoid X Receptor (Fxr) Modulatory Activity
      标题:Investigation On Bile Acid Receptor Regulators. Discovery Of Cholanoic Acid Derivatives With Dual G-Protein Coupled Bile Acid Receptor 1 (Gpbar1) Antagonistic And Farnesoid X Receptor (Fxr) Modulatory Activity
      摘要:Bile Acids,The End Products Of Cholesterol Metabolism,Activate Multiple Mechanisms Through The Interaction With Membrane G-Protein Coupled Receptors Including The Bile Acid Receptor Gpbar1 And Nuclear Receptors Such As The Bile Acid Sensor,Farnesoid X Receptor (Fxr). Even If Dual Fxr/gpbar1 Agonists Are Largely Considered A Novel Opportunity In The Treatment Of Several Liver And Metabolic Diseases,Selective Targeting Of One Of These Receptors Represents An Attractive Therapeutic Approach For A Wide Range Of Disorders In Which Dual Modulation Is Associated To Severe Side Effects. In The Present Study We Have Investigated Around The Structure Of Lca Generating A Small Library Of Cholane Derivatives,Endowed With Dual Fxr Agonism/gpbar1 Antagonism. To The Best Of Our Knowledge,This Is The First Report Of Bile Acid Derivatives Able To Antagonize Gpbar1. (C) 2015 Elsevier Inc. All Rights Reserved.
      DOI:10.1016/j.Steroids.2015.11.003

      海关参考信息

      专利信息


      专利号:US-9512167-B2
      优先权日:2010-11-30
      标 题 :Optimized synthesis of pure, non-polymorphic, crystalline bile acids with defined particle size
      发明人:WILHELM RUDOLF; PROELS MARKUS; FISCHER ERIK; WAENERLUND POULSEN HEIDI
      权利人:WILHELM RUDOLF; PROELS MARKUS; FISCHER ERIK; WAENERLUND POULSEN HEIDI; DR FALK PHARMA GMBH
      摘要:The present invention relates to a pure polymorph of Nor-UDCA or Bis-nor-UDCA, or of a pharmaceutically acceptable salt thereof. The invention further provides a pharmaceutical composition comprising the polymorph of the invention, and a method for preparing the polymorph. The invention includes the pharmaceutical use of the polymorph or of the pharmaceutical composition of the invention.

      专利号:US-2017057990-A1
      优先权日:2010-11-30
      标题 :Optimized Synthesis Of Pure, Non-Polymorphic, Crystalline Bile Acids With Defined Particle Size

      专利号:EP-2646457-A1
      优先权日:2010-11-30
      标 题:Optimized synthesis of pure, non-polymorphic, crystalline bile acids with defined particle size

      专利号:US-2014050791-A1
      优先权日:2010-11-30
      标 题 :Optimized Synthesis Of Pure, Non-Polymorphic, Crystalline Bile Acids With Defined Particle Size

      专利号:US-10000526-B2
      优先权日:2010-11-30
      标题 :Optimized synthesis of pure, non-polymorphic, crystalline bile acids with defined particle size

      专利号:US-4460509-A
      优先权日:1981-08-19
      标 题:Chemical synthesis
      发明人:MOSBACH ERWIN H; AYENGAR NARAYAN K N; MCSHERRY CHARLES K
      权利人:BETH ISRAEL MEDICAL CENTER
      摘要:This invention relates to steroid compounds having a D-ring side chain structure of the formula, wherein R1 may be or -CnH2n-, wherein n is an integer from 0 to 8; Y may be S, N, or O; x is and integer of from 1 to 3; and each Z may be the same or different and is selected from the group consisting of H, OH, alkyl, aryl, aralkyl, acyloxy, cycloalkyl, substituted alkyl, substituted aryl or substituted cycloalkyl.

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      合成参考文献


      参考文献:10.1023/b135931_1
      摘要:Kasal A. Structure and Nomenclature of Steroids. 2010. In: Steroid Analysis. : Springer Netherlands; 2010.
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