CAS: 3663-82-9; (2,3-Dihydrobenzo[b][1,4]Dioxin-2-yl)Methanol

上下游产品

ethyl 2,3-dihydro-1,4-benzodioxin-2-carboxylate benzene-1,2-diol glycerol epichlorohydrin 1,4,-benzodioxan-2-ylmethyl 4-acetoxyphenylacetate 2-(toluene-4-sulfonyloxymethyl)-2,3-dihydro-benzo[1,4]dioxine (S)-2-hydroxymethyl-1,4-benzodioxane 2-chloromethyl-1,4-benzodioxane

1,4-苯并二氧六环-2-甲酸乙酯置于lithium Aluminium Tetrahydride体系中,用 四氢呋喃 用作溶剂,化学反应生成2-羟基甲基-1,4-苯二恶
参考文献:卤素键增强了一系列双重5-Ht 6 / D 2配体的活性,这些配体是通过生物等位基因杂交/虚拟筛选方案设计的†
标题:卤素键增强了一系列双重5-Ht 6 / D 2配体的活性,这些配体是通过生物等位基因杂交/虚拟筛选方案设计的†
摘要:通过与在第二个靶标上具有活性的化合物的相似性相结合的化学空间变窄与化学空间缩小相结合的新型杂化生物等排体生成/虚拟筛选方法已成功地用于开发结构新的双5-Ht 6 / D 2受体配体.因此,合成了所发现的命中1D的一系列衍生物(n-[2-(二甲基氨基)乙基]-N-(2-苯基乙基)苯胺).最活跃的5-Ht 6 / D 2点的配体也显示出对5-Ht 7 R和5-Ht 2A R的对位-Chloroaniline衍生物被鉴定为一种有效的双重5-Ht 6 /5-Ht7受体拮抗剂( K I = 24 Nm和k B = 30 Nm,K I = 4 Nm和k B = 1.4 Nm).对于含卤素的化合物,在5-Ht 6,D 2和5-Ht 7受体上观测到了有趣的结构-活性关系,随后使用结合了量子极化的分子模型方法研究了配体-受体复合物配体对接(qpld)和分子力学通用出生/表面面积(mm / Gbsa)自由能计算,可以确定假定的卤素结合口袋.
Doi:10.1039/c6Ra08714K

专利信息

专利号:RU-2185379-C2
优先权日:1996-01-25
标 题:Method of stereoselective synthesis of heterobicyclic alcohol enantiomer, intermediate compounds and methods of their synthesis

专利号:RU-2124506-C1
优先权日:1992-12-21
标题:Method of stereoselective synthesis of heterobicyclic alcohol enantiomer, pure alcohol enantiomer, method of synthesis of piperazine derivative

专利号:US-4528195-A
优先权日:1978-02-01
标题:Imidazole derivatives and salts thereof, their synthesis and intermediates and pharmaceutical formulations
发明人：THOROGOOD PETER B
权利人:THOROGOOD PETER B
摘要:Pharmaceutical formulations comprising an imidazole (or pharmaceutically acceptable salt thereof) of formula: ##STR1## wherein (i) A is an aliphatic hydrocarbon residue of from 1 to 4 carbon atoms and R is a naphthyl, tetrahydronaphthyl, heterocyclyl, arylthio, arylalkylthio, aryloxy, arylalkyloxy, arylhydroxymethylene, arylcarbonyl, arylalkylcarbonyl, alkyloxy, alkylthio or a substituted cycloalkyl or cycloalkenyl group or n (ii) A is an --SO 2 -- group and R is aryl or heterocyclyl or n (iii) A is a chemical bond and R is a heterocyclyl or n Some of these imidazoles and salts are novel. n Methods of preparing the imidazoles are disclosed. The imidazoles and their salts are useful in the treatment or prophylaxis of thrombo-embolic conditions, shock and angina pectoris.

专利号:US-8178559-B2
优先权日:2004-12-30
标 题:Organic compounds
发明人：BREITENSTEIN WERNER; EHARA TAKERU; EHRHARDT CLAUS; GROSCHE PHILIPP; HITOMI YUKO; IWAKI YUKI; KANAZAWA TAKANORI; KONISHI KAZUHIDE; MAIBAUM JUERGEN KLAUS; MASUYA KEIICHI; IWASAKI ATSUKO; OSTERMANN NILS; SUZUKI MASAKI; TOYAO ATSUSHI; YOKOKAWA FUMIAKI
权利人:BREITENSTEIN WERNER; EHARA TAKERU; EHRHARDT CLAUS; GROSCHE PHILIPP; HITOMI YUKO; IWAKI YUKI; KANAZAWA TAKANORI; KONISHI KAZUHIDE; MAIBAUM JUERGEN KLAUS; MASUYA KEIICHI; IWASAKI ATSUKO; OSTERMANN NILS; SUZUKI MASAKI; TOYAO ATSUSHI; YOKOKAWA FUMIAKI; NOVARTIS AG
摘要:3,4-substituted piperidine compounds, these compounds for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease (=disorder) that depends on activity of renin; the use of a compound of that class for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on activity of renin; the use of a compound of that class in the treatment of a disease that depends on activity of renin; pharmaceutical formulations comprising a 3,4-substituted piperidine compound, and/or a method of treatment comprising administering a 3,4substituted piperidine compound, a method for the manufacture of a 3,4-substituted piperidine compound, and novel intermediates and partial steps for their synthesis are disclosed. The 3,4-disubstituted piperidine compounds have the formula (I), wherein the symbols have the meanings defined in the specification.