CAS: 2338-18-3; 2-Aminoindane Hydrochloride

上下游产品

indan-2-yl-carbamic acid ethyl ester indan-2-one oxime 2-azido-2,3-dihydro-1H-indene indan-2-ol (1S,2S)-trans-2-amino-1-indanol (1R,2R)-trans-2-amino-1-indanol 5-bromo-2-aminoindane N-indan-2-yl-acetamide

水合茚三酮置于硫酸,盐酸羟胺,溶剂黄146,Palladium 10% On Activated Carbon,氢气,盐酸体系中,用 乙醇 用作溶剂,25.0~55.0 °C,344.75 Kpa 条件下,反应 8.5H,以74%的收率获得2-氨基茚满盐酸盐
参考文献:2-氨基茚满盐酸盐生产新工艺的优化和放大
标题:2-氨基茚满盐酸盐生产新工艺的优化和放大
摘要:对生产 2-氨基茚满盐酸盐(制造新型生物活性分子的关键起始材料)的经济工艺的需求推动了使用廉价反应物茚三酮的新型合成路线的开发.该合成方法包括茚三酮肟化,然后催化还原生成的肟中间体得到 2-氨基茚满,并开发了一种产品纯化方案,以分离盐酸盐形式的 2-氨基茚满.随后的工艺开发通过识别快速和慢速反应的方式优化了还原步骤(分别对应于肟和二酮功能的还原),调整反应条件以在快速放热期间使用温和的条件,以确保工艺安全,随后为较慢的反应使用更严格的条件.该工艺在中试工厂成功扩大了 100 倍,在实验室和中试工厂之间具有出色的产量和产品质量一致性.
Doi:10.1021/op000222H

专利信息

专利号:WO-0010565-A1
优先权日:1998-08-18
标 题 :Growth hormone secretagogues
发明人：DODGE JEFFREY ALAN; HAUSER KENNETH LEE; HEIMAN MARK LOUIS; JONES SCOTT ALAN; ALT CHARLES ARTHUR; BRYANT HENRY UHLMAN; COHEN JEFFREY DANIEL; COPP JAMES DENSMORE; FAHEY KENNAN JOSEPH; GRITTON WILLIAM HARLAN; JUNGHEIM LOUIS NICKOLAUS; KENNEDY JOSEPH HENRY; LUGAR CHARLES WILLIS III; MUEHL BRIAN STEPHEN; PALKOWITZ ALAN DAVID; RATZ ANDREW MICHAEL; RHODES GARY ANTHONY; ROBEY ROBERT LEWIS; SEYLER DAVID EDWARD; SHEPHERD TIMOTHY ALAN; THRASHER KENNETH JEFF; TRANKLE WILLIAM GEORGE
权利人:LILLY CO ELI; DODGE JEFFREY ALAN; HAUSER KENNETH LEE; HEIMAN MARK LOUIS; JONES SCOTT ALAN; ALT CHARLES ARTHUR; BRYANT HENRY UHLMAN; COHEN JEFFREY DANIEL; COPP JAMES DENSMORE; FAHEY KENNAN JOSEPH; GRITTON WILLIAM HARLAN; JUNGHEIM LOUIS NICKOLAUS; KENNEDY JOSEPH HENRY; LUGAR CHARLES WILLIS III; MUEHL BRIAN STEPHEN; PALKOWITZ ALAN DAVID; RATZ ANDREW MICHAEL; RHODES GARY ANTHONY; ROBEY ROBERT LEWIS; SEYLER DAVID EDWARD; SHEPHERD TIMOTHY ALAN; THRASHER KENNETH JEFF; TRANKLE WILLIAM GEORGE
摘要:This invention relates to novel compounds which are useful in the modulation of endogenous growth hormone levels in a mammal. The invention further relates to novel intermediates for use in the synthesis of said compounds, as well as novel processes employed in these syntheses. Also included are methods of treating a mammal which include the administration of said compounds.

专利号:US-6992097-B2
优先权日:1998-08-18
标 题 :Growth hormone secretagogues
发明人：HAUSER KENNETH LEE; DODGE JEFFREY ALAN; HEIMAN MARK LOUIS; JONES SCOTT ALAN; ALT CHARLES ARTHUR; BRYANT HENRY UHLMAN; COHEN JEFFREY DANIEL; COPP JAMES DENSMORE; FAHEY KENNAN JOSEPH; GRITTON WILLIAM HARLAN; JUNGHEIM LOUIS NICKOLAUS; KENNEDY JOSEPH HENRY; LUGAR III CHARLES WILLIS; MUEHL BRIAN STEPHEN; PALKOWITZ ALAN DAVID; RATZ ANDREW MICHAEL; RHODES GARY ANTHONY; ROBEY ROGER LEWIS; SEYLER DAVID EDWARD; SHEPHERD TIMOTHY ALAN; THRASHER KENNETH JEFF; TRANKLE WILLIAM GEORGE
权利人:LILLY CO ELI
摘要:This invention relates to novel compounds which are useful in the modulation of endogenous growth hormone levels in a mammal. The invention further relates to novel intermediates for use in the synthesis of said compounds, as well as novel processes employed in these syntheses. Also included are methods of treating a mammal which include the administration of said compounds.

专利号:RU-2155761-C2
优先权日:1995-08-10
标题:Bicyclic derivatives of amidine, method of their synthesis, pharmaceutical composition and method of inhibition of nitrogen oxide synthetase activity

专利号:SK-10102003-A3
优先权日:2001-02-13
标题:Acylated indanylamines, a pharmaceutical composition thereof, a method of synthesis and their use as a medicament