Benzyl Indacaterol Hydrochloride置于palladium On Activated Charcoal,氢气,溶剂黄146体系中,用 甲醇 作为反应溶剂,25.0~30.0 °C,400.01 Kpa 条件下,反应 4.0H,以85.5%的收率获得产物茚达特罗 参考文献:Novel Process For Preparation Of Indacaterol Or Its Pharmaceutically Acceptable Salts 标题:Novel Process For Preparation Of Indacaterol Or Its Pharmaceutically Acceptable Salts 摘要:一种用于制备依那卡特罗或其药用可接受盐的新型工艺,以及用于制备该工艺的新型中间体,对于大规模生产具有经济意义.
专利号:US-2006167025-A1 优先权日:2004-12-22 标 题:Tricyclic amino alcohols, processes for synthesis of same and use of same as anti-inflammatory drugs 发明人:BERGER MARKUS; SCHMEES NORBERT; SCHAECKE HEIKE; BAURLE STEFAN; REHWINKEL HARTMUT; MENGEL ANNE; KROLIKIEWICZ KONRAD; GROSSBACH DANJA; VOIGTLAENDER DAVID 权利人:BERGER MARKUS; SCHMEES NORBERT; SCHAECKE HEIKE; BAURLE STEFAN; REHWINKEL HARTMUT; MENGEL ANNE; KROLIKIEWICZ KONRAD; GROSSBACH DANJA; VOIGTLAENDER DAVID 摘要:The invention relates to tricyclic amino alcohols of general formula (I) n nmethod for synthesis of same and use of same as anti-inflammatory agents.
专利号:US-10059653-B2 优先权日:2015-01-20 标 题 :Process for the preparation of indanamine derivatives and new synthesis intermediates 发明人:BERTOLINI GIORGIO; CEREA PAOLANGELO; COLLI CORRADO; FELICIANI LAZZARO; GASSA FEDERICO; BIANCHI ALDO; COLOMBO FEDERICA; MAIORANA STEFANO; NISIC FILIPPO 权利人:LABORATORIO CHIMICO INT S P A; OLON SPA 摘要:Subject-matter of the invention is a process for the preparation of a key intermediate in the synthesis of indacaterol. Subject-matter of the invention are also new synthesis intermediates. Formula (I):
专利号:US-10538479-B2 优先权日:2015-09-28 标题 :Process for the preparation of indanamine derivatives and new synthesis intermediates 发明人:COLLI CORRADO; AGOSTI ALESSANDRO; MAIORANA STEFANO; COLOMBO FEDERICA; BERTOLINI GIORGIO 权利人:OLON SPA 摘要:Subject-matter of the invention is a process for the preparation of key intermediates in the synthesis of indacaterol. Subject-matter of the invention are also new synthesis intermediates.
专利号:WO-2014139485-A1 优先权日:2013-03-15 标 题 :A method for the preparation of 5-[(r)-2-(5,6-diethyl-indan-2-ylamino)-l-hydroxyethyl]- 8-hydroxy-(1h)-quinolin-2-one (indacaterol) 发明人:MECA LUDEK; VANKOVA PAVLA 权利人:ZENTIVA KS 摘要:The invention relates to a new method of synthesis of 5-[( R )-2-(5,6-diethyl-indan-2-ylamino)- 1-hydroxyethyl]-8-hydroxy-(1 H )-quinolin-2-one of formula ( R )-2, known under the generic name indacaterol, which is used for the treatment of chronic obstructive pulmonary disease (COPD). The method comprises preparation of the racemic intermediate 5-[2-(5,6-diethyl-indan-2-ylamino)-1-hydroxyethyl]-8-benzyloxy-(1 H )-quinolin-2-one of formula 1, which is further, in an arbitrary order, chirally resolved and debenzylated, and subsequently indacaterol of formula ( R )-2 is isolated.
专利号:US-8697730-B2 优先权日:2007-10-26 标题 :5-lipoxygenase activating protein (FLAP) inhibitor 发明人:REWOLINSKI MELISSA VIRGINIA; SCHAAB KEVIN MURRAY; KING CHRISTOPHER DAVID; STOCK NICHOLAS SIMON 权利人:REWOLINSKI MELISSA VIRGINIA; SCHAAB KEVIN MURRAY; KING CHRISTOPHER DAVID; STOCK NICHOLAS SIMON; PANMIRA PHARMACEUTICALS LLC 摘要:Described herein are methods for the synthesis of 3-[5-(pyridin-2-ylmethoxy)-3-(2-methyl-2-propylthio)-1-[4-(2-methoxypyridin-5-yl)benzyl]-indol-2-yl]-2,2-dimethyl-propionic acid, pharmaceutically acceptable salts, pharmaceutically acceptable solvates thereof. Also described are pharmaceutical compositions suitable for oral administration to a mammal that include, as well as methods of using such oral pharmaceutical compositions for treating respiratory conditions or diseases, as well as other leukotriene-dependent or leukotriene mediated conditions or diseases.
专利号:US-2011118469-A1 优先权日:2009-11-04 标题 :Continuous flow synthesis of amino alcohols using microreactors
参考文献:10.2147/copd.s18529 摘要:Chapman KR, Fogarty CM, Peckitt C, Lassen C, Jadayel D, Dederichs J, Dalvi M, Kramer B. Delivery characteristics and patients' handling of two single-dose dry-powder inhalers used in COPD. Int J Chron Obstruct Pulmon Dis. 2011;6():353–63. 参考文献:10.1016/j.cct.2011.06.004 摘要:Stull DE, Wiklund I, Gale R, Capkun-Niggli G, Houghton K, Jones P. Application of latent growth and growth mixture modeling to identify and characterize differential responders to treatment for COPD. Contemp Clin Trials. 2011 Nov;32(6):818–28. doi: 10.1016/j.cct.2011.06.004. 参考文献:10.1016/j.rmed.2011.06.005 摘要:Price D, Gray A, Gale R, Asukai Y, Mungapen L, Lloyd A, Peters L, Neidhardt K, Gantner T. Cost-utility analysis of indacaterol in Germany: a once-daily maintenance bronchodilator for patients with COPD. Respir Med. 2011 Nov;105(11):1635–47. doi: 10.1016/j.rmed.2011.06.005.