CAS: 63676-22-2; 2-(4-Hydroxyphenyl)Benzo[b]Thiophen-6-Ol

上下游产品

CAS号63675-74-1 6-甲氧基-2-(4-甲氧苯基)苯并噻吩 | CAS号15570-12-4 3-甲氧基苯硫酚 | CAS号2632-13-5 4-甲氧基-α－溴代苯乙酮 | CAS号90560-10-4 6-甲氧基苯并噻吩 | CAS号182133-35-3 (6-甲氧基苯并[b]噻吩-2-基)硼酸 | CAS号63675-73-0 4-甲氧基-A-[(3-甲氧基... | CAS号84449-90-1 雷洛昔芬 | CAS号84449-63-8 2-[4-(乙酰氧基)苯基]苯... | CAS号84449-64-9 2-[4-(苯甲酰基氧基)苯基... | CAS号84449-65-0 2-[4-[(甲磺酰)氧]苯基... | CAS号63676-25-5 LY117018

Alpha-溴-4-甲氧基苯乙酮置于氢氧化钾,吡啶盐酸盐体系中,用 乙醇,水,乙酸乙酯 作为反应溶剂,化学反应 7.0H,反应生成 2-(4-羟基苯基)苯并[b]噻吩-6-醇
参考文献:抗雌激素.2.在一系列3-芳基-2-芳基苯并[b]噻吩衍生物中反应生成[6-羟基-2-(4-羟基苯基)苯并[b]噻吩-3-基] [4-[2-(1-哌啶基)乙氧基]-苯基]甲酮盐酸盐(ly156758),一种非常有效的雌激素拮抗剂,仅具有最小的内在雌激素性.
标题:抗雌激素.2.在一系列3-芳基-2-芳基苯并[b]噻吩衍生物中反应生成[6-羟基-2-(4-羟基苯基)苯并[b]噻吩-3-基] [4-[2-(1-哌啶基)乙氧基]-苯基]甲酮盐酸盐(ly156758),一种非常有效的雌激素拮抗剂,仅具有最小的内在雌激素性.
摘要:为了制备非甾体类抗雌激素,其显示出比目前可用的更高的拮抗作用和更低的内在雌激素性,合成了一系列3-芳基-2-芳基苯并[b]噻吩衍生物.这些化合物的制备方法是:将适当的o-保护的2-芳基苯并[b]噻吩核与带有碱性侧链的苯甲酰氯进行friedel-Crafts芳基化反应,然后去除保护基,以提供既包含羟基又包含碱性侧基的所需化合物.链功能.发现一种特别有用的裂解芳基甲氧基醚而不除去分子中其他地方的(二烷基氨基)乙氧基侧链官能度的方法是alcl 3 / Etsh.测试了苯并噻吩衍生物抑制雌二醇对未成熟大鼠子宫的生长刺激作用的能力.看来侧链胺部分的微小变化对化合物拮抗雌二醇的能力有深远的影响.发现具有包含环(吡咯烷,哌啶和六亚甲基胺)部分的碱性侧链的类似物具有比其非环状对应物更少的固有雌激素性并且更完全地拮抗雌二醇的作用.该系列中最有效的抗雌激素化合物,化合物44,[6-羟基-2-(4-羟基苯基)苯并[b]噻吩-3-基]-[4-
DOI:10.1021/jm00374A021

专利信息

专利号:US-6372945-B1
优先权日:1995-06-07
标 题 :Process for the synthesis of vinyl sulfoxides
发明人：AIKINS JAMES A; MILLER RANDAL SCOT; ZHANG TONY Y
权利人:LILLY CO ELI
摘要:The present invention is directed to a new process for the synthesis of vinyl sulfoxides, in particular diarylvinyl sulfoxides

专利号:US-5606076-A
优先权日:1995-06-07
标 题 :Process for the synthesis of benzo[b]thiophenes
发明人：AIKINS JAMES A; ZHANG TONY Y
权利人:LILLY CO ELI
摘要:The present invention is directed to a process for the synthesis of 2-arylbenzo[b]thiophenes.

专利号:US-5569772-A
优先权日:1995-06-07
标 题:Process for the synthesis of benzo[b]thiophenes
发明人：HOARD DAVID W; LUKE WAYNE D
权利人:LILLY CO ELI
摘要:The present invention is directed to a new process for the synthesis of 2-aryl benzo[b]thiophenes, and to novel intermediates therefor.

专利号:US-5606075-A
优先权日:1995-06-07
标 题:Process for the synthesis of benzo[b]thiophenes
发明人：HOARD DAVID W; LUKE WAYNE D
权利人:LILLY CO ELI
摘要:The present invention is directed to new processes for the synthesis of 2-aryl benzo[b]thiophenes.

专利号:US-6472531-B1
优先权日:1994-09-19
标题 :Synthesis of 3-[4-(2-aminoethoxy)-benzoyl]-2-aryl-6-hydroxybenzo[b]thiophenes
发明人：LABELL ELIZABETH SMITH; MCGILL JOHN MCNEILL; MILLER RANDAL SCOT
权利人:LILLY CO ELI
摘要:The present invention is directed to chemical processes for preparing 2-aryl-6-hydroxy-3-[4-(2-aminoethoxy)benzoyl]benzo[b]-thiophenes. The present invention is also directed to crystalline solvates and a non-solvated crystalline form of 6-hydroxy-2-(4-hydroxyphenyl)-3-[4-(2-piperidinoethoxy)benzoyl]-benzo[b]thiophene hydrochloride, as well as processes for their preparation.

专利号:US-2005054770-A1
优先权日:2001-03-09
标题 :Helicomimetics and stabilized lxxll peptidomimetics
发明人：SPATOLA ARNO F; SPATOLA JACKIE B; LEDUC ANNE-MARIE
摘要:This invention pertains to the design and synthesis of molecules that can act as protein mimics. In particular this disclosure teaches the preparation of short, cyclic peptide sequences that can adopt a helical conformation and display a particular arrangement of amino acid side chains oriented in a specific arrangement to serve as a pharmacophore. A ring, formed by a disulfide bridge between pairs of cysteine residues, maintains the helical structure. When the cysteines are arranged in a pattern of i to i+3 as illustrated in FIG. 1 , and when the first cysteine is of the D-configuration, and the second cysteine is of the L-configuration, the helical arrangement is especially stabilized. A preferred version of this invention involves a pentapeptide sequence of general structure known as the NR Box, stabilized by a side chain to side chain disulfide bridge formed from the two cysteines.