CAS: 263717-53-9; 4,4',4''-(4-Propyl-1H-Pyrazole-1,3,5-Triyl)Triphenol

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4-N-Propyl-1-(4-Methoxyphenyl)-3,5-Bis(4-Methoxyphenyl)Pyrazole 263717-52-8

📜4-甲氧基苯肼盐酸盐置于三溴化硼体系中,用 四氢呋喃,二氯甲烷,N,N-二甲基甲酰胺 用作溶剂,化学反应生成4,44''-(4-丙基-[1H]-吡唑-1,3,5-三基)三酚
参考文献:Pyrazole Ligands: Structure−affinity/activity Relationships And Estrogen Receptor-α-Selective Agonists
标题:Pyrazole Ligands: Structure−affinity/activity Relationships And Estrogen Receptor-α-Selective Agonists
摘要:We Have Found That Certain Tetrasubstituted Pyrazoles Are High-Affinity Ligands For The Estrogen Receptor (Er) (Fink Et Al. Chem. Biol. 1999,6,205-219) And That One Pyrazole Is Considerably More Potent As An Agonist On The Er Alpha Than On The Er Beta Subtype (Sun Et Al. Endocrinology 1999,140,800-804). To Investigate What Substituent Pattern Provides Optimal Er Binding Affinity And The Greatest Enhancement Of Potency As An Er Alpha-Selective Agonist,We Prepared A Number Of Tetrasubstituted Pyrazole Analogues With Defined Variations At Certain Substituent Positions. Analysis Of Their Binding Affinity Pattern Shows That A C(4)-Propyl Substituent Is Optimal And That A P-Hydroxyl Group On The N(1)-Phenyl Group Also Enhances Affinity And Selectivity For Er Alpha. The Best Compound In This Series,A Propylpyrazole Triol (Ppt,Compound 4G),Binds To Er Alpha With High Affinity (Ca. 50% That Of Estradiol),And It Has A 410-Fold Binding Affinity Preference For Er Alpha. It Also Activates Gene Transcription Only Through Er Alpha. Thus,This Compound Represents The First Er Alpha-Specific Agonist. We Investigated The Molecular Basis For The Exceptional Er Alpha Binding Affinity And Potency Selectivity Of Pyrazole 4G By A Further Study Of Structure-Affinity Relationships In This Series And By Molecular Modeling. These Investigations Suggest That The Pyrazole Triols Prefer To Bind To Er Alpha With Their C(3)-Phenol In The Estradiol A-Ring Binding Pocket And That Binding Selectivity Results From Differences In The Interaction Of The Pyrazole Core And C(4)-Propyl Group With Portions Of The Receptor Where Er Alpha Has A Smaller Residue Than Er Beta. These Er Subtype-Specific Interactions And The Er Subtype-Selective Ligands That Can Be Derived From Them Should Prove Useful In Defining Those Biological Activities In Estrogen Target Cells That Can Be Selectively Activated Through Er Alpha.
Doi:10.1021/jm000170M

专利信息

专利号:US-6924375-B2
优先权日:2003-09-03
标题:Facile synthesis of 1,9-diacyldipyrromethanes
发明人：LINDSEY JONATHAN S; TAMARU SHUN-ICHI; YU LIANHE
权利人:UNIV NORTH CAROLINA STATE
摘要:The present invention provides a method of making a metal complex. The method comprises the steps of: (a) acylating a dipyrromethane or a 1-monoacyldipyrromethane to form a mixed reaction product comprising a 1,9-diacyidipyrromethane; (b) combining the reaction product with a compound of the formula R 2 MX 2 in the presence of a base, where R is alkyl or aryl, M is Sn, Si, Ge, or Pb (preferably Sn), and X is halo, OAc, acac, or OTf, to form a product comprising a metal complex of the formula DMR 2 in the mixed reaction product, wherein D is a 1,9-diacyldipyrromethane; and then (c) separating the metal complex from the mixed reaction product. The method may be utilized for the convenient synthesis and separation of 1,9-diacyldipyrromethanes. Metal complex intermediates useful in such methods are also described.

专利号:EP-0224088-A2
优先权日:1985-11-28
标题 :Process for the solid-phase synthesis of retro-inverso peptides

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优先权日:2021-08-23
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