CAS: 114772-38-2; Methyl 2-[4-(Bromomethyl)Phenyl]Benzoate

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CAS号114772-34-8 2-(对甲苯基)苯甲酸甲酯 | CAS号158144-55-9 2-(4-Hydroxymet... | CAS号34241-39-9 2-(2-cyanopropa... | CAS号128-08-5 N-溴代丁二酰亚胺 | CAS号7148-03-0 2-(对甲苯基)苯甲酸 | CAS号5720-05-8 对甲基苯基硼酸 | CAS号88-65-3 邻溴苯甲酸 | CAS号624-31-7 对碘甲苯 | CAS号610-97-9 邻碘苯甲酸甲酯 | CAS号57598-33-1 2-(2-甲氧基苯基)-4,4... | CAS号528560-93-2 4'-[[[2-正丙基-4-甲... | CAS号144701-48-4 替米沙坦 | CAS号114798-32-2 2-[4-[[2-but-1-...

2-溴苯甲酸置于n-溴代丁二酰亚胺(Nbs),硫酸,Palladium Diacetate,过氧化苯甲酰体系中,用 四氯化碳,水 用作溶剂,化学反应 14.08H,反应生成4'-溴甲基-2-甲酸甲酯联苯
参考文献:New Telmisartan-Derived Pparγ Agonists: Impact Of The 3D-Binding Mode On The Pharmacological Profile
标题:New Telmisartan-Derived Pparγ Agonists: Impact Of The 3D-Binding Mode On The Pharmacological Profile
摘要:In Previous Studies,The 4'-((2-Propyl-1H-Benzo[d]Imidazol-1-Yemethyl)-[1,1'-Biphenyl]-2-Carboxylic Acid Was Identified As Pharmacophoric Core For Ppar Gamma Activation. In This Structure-Activity Relationship Study The C2-Alkyl Chain Was Elongated And The 2-Cooh Group Was Changed To A Carbamide/carbonitrile Or Shifted To The 3-Or 4-Position. Furthermore,The Benzo[d]Imidazole Was Exchanged By 2,3Dihydrobenzo[d]Thiazole Or 1H-Indole. C2-Propyl Derivatives Showed The Profile Of Partial Agonists,While Elongation Of The C2-Chain To That Of An N-Heptyl Group Or A 4-Cooh Shift Changed The Pharmacological Profile To That Of A Potent Full Agonist. This Finding Can Be Explained By Binding To The Lbd In Different Ligand Conformations. Two Anchoring Points (Tyr473 And Arg288) Exist In The Lbd,Which Have To Be Contacted To Achieve Receptor Activation. In A Crystal Violet Chemosensitivity Assay Using Cos-7 Cells And Lncap Cells Expressing Ppar Gamma Only The Carbamide Derivatives Influenced The Cell Growth,Independently On The Presence Of The Ppar Gamma. Therefore,Receptor Mediated Cytotoxicity Can Be Excluded. (C) 2016 Elsevier Masson Sas. All Rights Reserved.
Doi:10.1016/j.Ejmech.2016.08.027

专利信息

专利号:US-10077242-B2
优先权日:2014-12-01
标题 :Convergent approach to the total synthesis of telmisartan via a suzuki cross-coupling reaction
发明人：GUPTON FRANK; MARTIN ALEX; SIAMAKI ALI; BELECKI KATHERINE
权利人:UNIV VIRGINIA COMMONWEALTH
摘要:Methods of synthesizing the angiotensin II receptor antagonist telmisartan in high yield and purity are provided. The methods involve the coupling of two structurally distinct benzimidazole units via a Suzuki cross-coupling reaction. Methods of regioselectively synthesizing one of the benzimidazole units are also provided.

专利号:US-7968727-B2
优先权日:2005-04-01
标 题 :Synthesis of 4-bromomethyl-2′-formylbiphenyl and 4-bromomethyl-2′-hydroxymethylbiphenyl and its use in preparation of angiotensin II antagonists
发明人：COPAR ANTON; ANTONCIC LJUBOMIR; ANTONCIC MATEJ
权利人:LEK PHARMACEUTICALS
摘要:4-bromomethyl-2′-formylbiphenyl and 4-bromomethyl-2′-hydroxymethylbiphenyl are useful starting material for the preparation various angiotenzin II antagonists, which are prepared from 4-bromomethyl-2′-cyanobiphenyl or 4′-bromomethylbiphenylcarboxyilic derivatives using selected hydride reagent.

专利号:US-2009318521-A1
优先权日:2005-04-01
标题 :Synthesis of 4-Bromomethyl-2'-Formylbiphenyl and 4-Bromomethyl-2'-Hydroxymethylbiphenyl and Its Use in Preparation of Giotensin II Antagonists

专利号:RU-2023713-C1
优先权日:1989-12-18
标 题:Method of synthesis of benzimidazole derivatives or their salts

专利号:WO-2006103068-A1
优先权日:2005-04-01
标题:A synthesis of 4-bromomethyl-2'-formylbiphenyl and 4-bromomethyl-2'- hydroxymethylbiphenyl and its use in preparation of angiotensin ii antagonists

专利号:US-2017260146-A1
优先权日:2014-12-01
标题 :A convergent approach to the total synthesis of telmisartan via a suzuki cross-coupling reaction