CN102939285A - 5-[[2(r)-[1(r)-[3,5-双(三氟甲基)苯基]乙氧基]-3(s)-4-(氟苯基)-4-吗啉基]甲基]-1,2-二氢-3h-1,2,4-三唑-3-酮的制备方法 - Google Patents

5-[[2(r)-[1(r)-[3,5-双(三氟甲基)苯基]乙氧基]-3(s)-4-(氟苯基)-4-吗啉基]甲基]-1,2-二氢-3h-1,2,4-三唑-3-酮的制备方法 Download PDF

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CN102939285A
CN102939285A CN2011800227753A CN201180022775A CN102939285A CN 102939285 A CN102939285 A CN 102939285A CN 2011800227753 A CN2011800227753 A CN 2011800227753A CN 201180022775 A CN201180022775 A CN 201180022775A CN 102939285 A CN102939285 A CN 102939285A
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morpholinyl
fluorophenyl
triazole
dihydro
trifluoromethyl
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CN102939285B (zh
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姬建新
张强
杜锋田
金毅
张涛
郭娜
严小威
杨永荣
李伯刚
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Chengdu Diao Pharmaceutical Group Co Ltd
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Chengdu Diao Pharmaceutical Group Co Ltd
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D265/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
    • C07D265/28—1,4-Oxazines; Hydrogenated 1,4-oxazines
    • C07D265/30—1,4-Oxazines; Hydrogenated 1,4-oxazines not condensed with other rings
    • C07D265/32—1,4-Oxazines; Hydrogenated 1,4-oxazines not condensed with other rings with oxygen atoms directly attached to ring carbon atoms

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

本发明公开了式Ⅰ化合物5-[[2(R)-[1(R)-[3,5-双(三氟甲基)苯基]乙氧基]-3(S)-4-(氟苯基)-4-吗啉基]甲基]-1,2-二氢-3H-1,2,4-三唑-3-酮（即，阿瑞匹坦）的合成方法，所述方法包括在溶剂中环合式4化合物，其中R是C1-C5烷基。还公开了制备阿瑞匹坦的中间化合物。所述方法特别适用于阿瑞匹坦的工业化生产。

Description

PCT国内申请，说明书已公开。

Claims (1)

  1. PCT国内申请，权利要求书已公开。
CN201180022775.3A 2010-05-24 2011-05-20 5-[[2(r)-[1(r)-[3,5-双(三氟甲基)苯基]乙氧基]-3(s)-4-(氟苯基)-4-吗啉基]甲基]-1,2-二氢-3h-1,2,4-三唑-3-酮的制备方法 Active CN102939285B (zh)

Priority Applications (1)

Application Number Priority Date Filing Date Title
CN201180022775.3A CN102939285B (zh) 2010-05-24 2011-05-20 5-[[2(r)-[1(r)-[3,5-双(三氟甲基)苯基]乙氧基]-3(s)-4-(氟苯基)-4-吗啉基]甲基]-1,2-二氢-3h-1,2,4-三唑-3-酮的制备方法

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
CN201010181849.5 2010-05-24
CN201010181849 2010-05-24
PCT/CN2011/074372 WO2011147279A1 (zh) 2010-05-24 2011-05-20 5-[[2(r)-[1(r)-[3,5-双(三氟甲基)苯基]乙氧基]-3(s)-4-(氟苯基)-4-吗啉基]甲基]-1,2-二氢-3h-1,2,4-三唑-3-酮的制备方法
CN201180022775.3A CN102939285B (zh) 2010-05-24 2011-05-20 5-[[2(r)-[1(r)-[3,5-双(三氟甲基)苯基]乙氧基]-3(s)-4-(氟苯基)-4-吗啉基]甲基]-1,2-二氢-3h-1,2,4-三唑-3-酮的制备方法

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CN201110131894.4A Active CN102295611B (zh) 2010-05-24 2011-05-20 一种神经激肽1受体拮抗剂类药物的合成方法
CN201180022775.3A Active CN102939285B (zh) 2010-05-24 2011-05-20 5-[[2(r)-[1(r)-[3,5-双(三氟甲基)苯基]乙氧基]-3(s)-4-(氟苯基)-4-吗啉基]甲基]-1,2-二氢-3h-1,2,4-三唑-3-酮的制备方法

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Publication number Priority date Publication date Assignee Title
PT2817305T (pt) * 2012-02-23 2016-11-02 Piramal Entpr Ltd Um processo melhorado para a preparação de aprepitant
CZ304770B6 (cs) * 2012-03-13 2014-10-08 Zentiva, K.S. Způsob výroby 3-(((2R,3S)-2-((R)-1-(3,5-bis(trifluormethyl)fenyl)ethoxy)-3-(4-fluorfenyl)morfolino)methyl)-1H-1,2,4-triazol-5(4H)-onu (Aprepitantu) v polymorfní formě II
CN103193725A (zh) * 2013-04-12 2013-07-10 上海医药工业研究院 (2r,3r)-2-[(1r)-1-[3,5-双(三氟甲基)苯基]乙氧基]-3-(4-氟苯基)吗啉盐的制法
CN103694146B (zh) * 2013-12-04 2015-10-28 深圳万乐药业有限公司 2-(2-氯-1-亚乙基)酰肼甲酸甲酯的制备方法

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CN1646525A (zh) * 2002-04-18 2005-07-27 麦克公司 5－[[2(r)－[1(r)－[3,5－双(三氟甲基)苯基]乙氧基]－3(s)－(4－氟苯基)－4－吗啉基]甲基]－1,2－二氢－3h－1,2，4－三唑－3－酮的制备方法
WO2007039883A2 (en) * 2005-10-05 2007-04-12 Ranbaxy Laboratories Limited Process for preparation of aprepitant

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US5719147A (en) 1992-06-29 1998-02-17 Merck & Co., Inc. Morpholine and thiomorpholine tachykinin receptor antagonists
ZA985765B (en) 1997-07-02 1999-08-04 Merck & Co Inc Polymorphic form of a tachykinin receptor antagonist.
WO2007044829A2 (en) 2005-10-06 2007-04-19 Dr. Reddy's Laboratories Ltd. Preparation of aprepitant
WO2009001203A2 (en) * 2007-06-27 2008-12-31 Orchid Chemicals & Pharmaceuticals Limited An improved process for the preparation of aprepitant
WO2009116081A2 (en) * 2008-03-03 2009-09-24 Msn Laboratories Limited An improved process for the preparation of aprepitant
WO2010092591A2 (en) * 2008-06-30 2010-08-19 Usv Limited Novel crystalline polymorphs of 5-[[(2r,3s)-2-[(1r)-1-[3,5- bis(trifluoromethyl) phenyl] ethoxy]-3-(4-fluorophenyl)-4-morpholinyl]methyl]-1,2- dihydro-3h-1,2,4-triazol-3-one and process for preparation thereof

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1646525A (zh) * 2002-04-18 2005-07-27 麦克公司 5－[[2(r)－[1(r)－[3,5－双(三氟甲基)苯基]乙氧基]－3(s)－(4－氟苯基)－4－吗啉基]甲基]－1,2－二氢－3h－1,2，4－三唑－3－酮的制备方法
WO2007039883A2 (en) * 2005-10-05 2007-04-12 Ranbaxy Laboratories Limited Process for preparation of aprepitant

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
KAREL M. J. BRANDS等: "Efficient Synthesis of NK1 Receptor Antagonist Aprepitant Using a Crystallization-Induced Diastereoselective Transformation", 《JOURNAL OF THE AMERICAN CHEMICAL SOCIETY》, vol. 125, no. 8, 30 January 2003 (2003-01-30), pages 2129 - 2135, XP 002374343, DOI: doi:10.1021/ja027458g *

Also Published As

Publication number Publication date
CN102939285B (zh) 2014-12-24
US8940890B2 (en) 2015-01-27
CN102295611B (zh) 2014-09-10
US20130109853A1 (en) 2013-05-02
CN102295611A (zh) 2011-12-28
WO2011147279A1 (zh) 2011-12-01

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