CAS: 4335-77-7; 2-Cyclohexyl-2-Hydroxy-2-Phenylacetic Acid

上下游产品

CAS号31197-69-0 2-环己基-2-羟基苯乙酸乙酯 | CAS号10399-13-0 2-环己基-2-羟基苯乙酸甲酯 | CAS号424792-60-9 2-(2'-cyclohexe... | CAS号424792-59-6 methyl 2-(2'-cy... | CAS号76-93-7 二苯乙醇酸 | CAS号1603-79-8 苯甲酰甲酸乙酯 | CAS号931-50-0 环己基溴化镁 | CAS号4358-87-6 DL-扁桃酸甲酯 | CAS号1508-65-2 盐酸奥昔布宁 | CAS号108-85-0 溴代环己烷 | CAS号5633-20-5 奥昔布宁 | CAS号712-50-5 环己基苯基酮 | CAS号10399-13-0 2-环己基-2-羟基苯乙酸甲酯 | CAS号52034-92-1 二环己基乙酸 | CAS号50-10-2 奥芬溴铵 | CAS号7146-19-2 2-(1-methyl-3,4... | CAS号6313-70-8 Acide dicyclohe... | CAS号3894-09-5 α-环己基苯乙酸

二苯基羟基乙酸置于platinum(Iv) Oxide 氢气,溶剂黄146体系中,80.0 °C,413.68 Kpa 条件下,反应 28.0H,反应生成 2-环己基-2-羟基苯乙酸
参考文献:Synthesis,Antimuscarinic Activity And Quantitative Structure-Activity Relationship (Qsar) Of Tropinyl And Piperidinyl Esters.
标题:Synthesis,Antimuscarinic Activity And Quantitative Structure-Activity Relationship (Qsar) Of Tropinyl And Piperidinyl Esters.
摘要:一系列トロピニル(tropinyl)およびピペリジニル(piperidinyl)エステルが合成され,ラット(m3)およびウサギ(m2)大動脈の内皮ムスカリン受容体に対する阻害活性が評価された.いくつかのエステル(シクロヘキシルフェニルグリコレートおよびシクロヘキシルフェニルプロピオネート)は,標準的なm2およびm3阻害剤であるafdx116および4-ジフェニルアセトキシ-N-メチルピペリジン(damp)よりも優れた抗ムスカリン化合物であり,Pkec50値は8-9の範囲であった.いくつかのエステルはm2よりもm3阻害剤としてより選択的であることが判明したが,これらは活性が低い傾向にあった.これらのエステルの親水性,電子的および立体特性は,親水性(HPLC容量係数,Log Kw),サイズ(分子体積)および電子的特性(taftの極性置換基定数σ*および13C化学シフト差δδ)を表す適切なパラメータを用いて抗ムスカリン活性と相関づけられた.最後に,エステルのm2阻害活性の92%は側鎖のサイズおよび電子的特性σ*によって説明できた.対照的に,これらのエステルのm3阻害活性は主に側鎖の電子的性質(σ*,δδ)によるものであり,優れた活性は電子引き抜き基に関連していた.比較分子場分析(comfa)の立体および静電場の可視化は,従来の定量的構造活性相関(qsar)アプローチから導出された構造活性相関(sar)のさらなる確認を提供した.
DOI:10.1248/cpb.46.231

专利信息

专利号:US-6825378-B2
优先权日:2003-03-28
标 题 :Process for the synthesis of enantiomerically pure cyclohexylphenyl glycolic acid
发明人：KUMAR PRADEEP; FERNANDES RODNEY AGUSTINHO; GUPTA PRITI
权利人:COUNCIL SCIENT IND RES
摘要:The present invention provides a process for the synthesis of enantiomerically pure cyclohexylphenyl glycolic acid of formula (1). The present invention more particularly relates to a process using cyclohexylphenyl ketone for the synthesis of enantiomerically pure cyclohexylphenyl glycolic acid of formula (1).

专利号:US-6140529-A
优先权日:1998-10-22
标 题 :Synthesis of optically active cyclohexylphenylglycolate esters
发明人：BAKALE ROGER P; LOPEZ JORGE L; MCCONVILLE FRANCIS X; VANDENBOSSCHE CHARLES P; SENANAYAKE CHRIS HUGH
权利人:SEPRACOR INC
摘要:A process for the preparation of optically active cyclohexylphenylglycolate esters is described. The process utilizes carboxylic acid activation to couple (R)- or (S)-cyclohexylphenylglycolic acid (CHPGA) with 4-N,N-diethylamino butynol or other propargyl alcohol derivatives. The preparation of the hydrochloride salt is also described. In addition, a resolution process employing tyrosine methyl ester enantiomers for preparing a single enantiomer of CHPGA from racemic CHPGA is disclosed.

专利号:US-7816375-B2
优先权日:2000-09-11
标 题 :Ligands for monoamine receptors and transporters, and methods of use thereof
发明人：AQUILA BRIAN M; BANNISTER THOMAS D; CUNY GREGORY D; HAUSKE JAMES R; HOLLAND JOANNE M; PERSONS PAUL E; RADEKE HEIKE; WANG FENGJIANG; SHAO LIMING
权利人:SEPRACOR INC
摘要:One aspect of the present invention relates to heterocyclic compounds. A second aspect of the present invention relates to the use of the heterocyclic compounds as ligands for various mammalian cellular receptors, including dopamine, serotonin, or norepinephrine transporters. The compounds of the present invention will find use in the treatment of numerous ailments, conditions and diseases which afflict mammals, including but not limited to addiction, anxiety, depression, sexual dysfunction, hypertension, migraine, Alzheimer's disease, obesity, emesis, psychosis, schizophrenia, Parkinson's disease, inflammatory pain, neuropathic pain, Lesche-Nyhane disease, Wilson's disease, and Tourette's syndrome. An additional aspect of the present invention relates to the synthesis of combinatorial libraries of the heterocyclic compounds, and the screening of those libraries for biological activity, e.g., in assays based on dopamine transporters.

专利号:US-2010184989-A1
优先权日:2007-03-12
标 题 :De Novo Synthesis of Conjugates
发明人：RIGGS-SAUTHIER JENNIFER; DENG BO-LIANG; REN ZHONGXU; ZHANG WEN; GU XUYUAN; DUARTE FRANCO J
权利人:NEKTAR THERAPEUTICS
摘要:The invention provides methods for the preparation of small molecule drugs that are chemically modified by covalent attachment of a water-soluble oligomer obtained from a water-soluble oligomer composition. Such drugs are produced through modification of a synthetic pathway to attach the oligomer to an intermediate compound followed by completion of the synthetic path.

专利号:AU-2008226820-A1
优先权日:2007-03-12
标题 :De novo synthesis of conjugates

专利号:CA-2679473-A1
优先权日:2007-03-12
标题:De novo synthesis of conjugates