Synthesis of Tetracyclic Heterocompounds as Selective Estrogen Receptor Modulators. Part 3. Development of an Acid-Catalyzed Racemization Process for (S)-2,8-(Dimethoxy)-5-{4-[2-(1-piperidinyl)ethoxy]- phenyl}-11,12-dihydro-5H-6,13-dioxabenzo[3,4]cyclohep.

Xun Li; Ronald K. Russell; Andras Horvath

首页> 外文期刊>Organic process research & development >Synthesis of Tetracyclic Heterocompounds as Selective Estrogen Receptor Modulators. Part 3. Development of an Acid-Catalyzed Racemization Process for (S)-2,8-(Dimethoxy)-5-{4-[2-(1-piperidinyl)ethoxy]- phenyl}-11,12-dihydro-5H-6,13-dioxabenzo[3,4]cyclohep.

【24h】

Synthesis of Tetracyclic Heterocompounds as Selective Estrogen Receptor Modulators. Part 3. Development of an Acid-Catalyzed Racemization Process for (S)-2,8-(Dimethoxy)-5-{4-[2-(1-piperidinyl)ethoxy]- phenyl}-11,12-dihydro-5H-6,13-dioxabenzo[3,4]cyclohep.

机译：四环杂化合物的合成作为选择性雌激素受体调节剂。第3部分。（S）-2,8-（二甲氧基）-5- {4- [2- [2-（1-哌啶基）乙氧基]-苯基} -11,12-dihydro-5H的酸催化外消旋方法的发展-6，13-二氧杂苯并[3，4]环庚。

获取原文

获取原文并翻译 | 示例

掌桥外文数据库（机构版） >>

开具论文收录证明 >>

文献代查 >>

页面导航

摘要
著录项
相似文献
相关主题

摘要

A novel and economical process was developed for recycling the undesired enantiomer, (S)-2,8-dimethoxy-5-{4-[2-(1-piperidinyl)-ethoxy]phenyl}-11,12-dihydro-5H-6,13-dioxabenzo[3,4]cyclohep-ta[1,2-a]naphthalene (1b) obtained from chiral chromatographic separation, by refluxing 1b with HCl (4.0 equiv) in EtOH for 76 h, or with H2SO4 (2.0 equiv) in water for 68 h to afford a near racemic mixture ((R)-1a/(S)-1b = 41-42%/49-53%, chiral HPLC area%) in >96% isolated yield and good chemical purity (87-95%).

机译：开发了一种新颖且经济的方法来回收不需要的对映异构体（S）-2,8-二甲氧基-5- {4- [2- [1-（1-哌啶基）-乙氧基]苯基} -11,12-二氢-5H-通过手性色谱分离，通过将1b与HCl（4.0当量）在EtOH中回流76 h，或与H2SO4（2.0）回流得到的6,13-二氧杂苯并[3,4]环庚-ta [1,2-a]萘（1b）当量）在水中反应68小时，得到接近外消旋的混合物（（R）-1a /（S）-1b = 41-42％/ 49-53％，手性HPLC面积％），分离产率> 96％，化学性质良好纯度（87-95％）。

著录项

来源
《Organic process research & development》 |2009年第1期|共4页
作者
Xun Li; Ronald K. Russell; Andras Horvath;
展开▼
作者单位

展开▼
收录信息
原文格式 PDF
正文语种 eng
中图分类有机化学;
关键词

相似文献

外文文献
中文文献
专利

1. Synthesis of Tetracyclic Heterocompounds as Selective Estrogen Receptor Modulators. Part 3. Development of an Acid-Catalyzed Racemization Process for (S)-2,8-(Dimethoxy)-5-{4-[2-(1-piperidinyl)ethoxy]- phenyl}-11,12-dihydro-5H-6,13-dioxabenzo[3,4]cyclohep. [J] . Xun Li, Ronald K. Russell, Andras Horvath Organic process research & development . 2009,第1期

机译：四环杂化合物的合成作为选择性雌激素受体调节剂。第3部分。（S）-2,8-（二甲氧基）-5- {4- [2- [2-（1-哌啶基）乙氧基]-苯基} -11,12-dihydro-5H的酸催化外消旋方法的发展-6，13-二氧杂苯并[3，4]环庚。
2. Synthesis of tetracyclic heterocompounds as selective estrogen receptor modulators. Part 1. Process development for scale-up of 2,5,8-substituted 5,11-dihydrochromeno[4,3-c]chromene derivatives [J] . Li X, Reuman M, Russell RK, Organic process research & development . 2007,第3期

机译：四环杂化合物的合成作为选择性雌激素受体调节剂。第1部分。扩大2,5,8-取代的5,11-二氢色酚[4,3-c]色烯衍生物的工艺开发
3. Convenient Synthesis and Structural Characterization of a Series of Methyl 4-[2-(cyclized amino)ethoxy]benzoate Esters as Key Intermediates in Synthesis of Selective Estrogen Receptor Modulators. [J] . Maha Aboul Ela, Doaa AE Issa, Farah H Mansour Medicinal Chemistry . 2018,第8期

机译：一系列4- [2-（环化氨基）乙氧基]苯甲酸甲酯作为选择性雌激素受体调节剂合成的关键中间体的简便合成和结构表征。

Synthesis of Tetracyclic Heterocompounds as Selective Estrogen Receptor Modulators. Part 3. Development of an Acid-Catalyzed Racemization Process for (S)-2,8-(Dimethoxy)-5-{4-[2-(1-piperidinyl)ethoxy]- phenyl}-11,12-dihydro-5H-6,13-dioxabenzo[3,4]cyclohep.

摘要

著录项

相似文献

相关主题

期刊订阅