Expeditious synthesis of novel NK1 antagonists based on a 1,2,4-trisubstituted cyclohexane

被引:8
|
作者
Dirat, O [1 ]
Elliott, JM [1 ]
Jelley, RA [1 ]
Jones, AB [1 ]
Reader, M [1 ]
机构
[1] Merck Sharp & Dohme Res Labs, Ctr Res Neurosci, Dept Med Chem, Harlow CM20 2QR, Essex, England
关键词
NK1; asymmetric synthesis; triazole; alpha-arylation;
D O I
10.1016/j.tetlet.2005.12.067
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
A stereoselective asymmetric route to novel potent NK1 antagonists based on a 1.2,4-trisubstituted cyclohexane core is discussed. (c) 2005 Elsevier Ltd. All rights reserved.
引用
收藏
页码:1295 / 1298
页数:4
相关论文
共 50 条
  • [21] A facile and efficient method for the synthesis of 1,2,4-trisubstituted imidazoles with enamides and benzylamines
    Cao, Jinhui
    Zhou, Xiaoqiang
    Ma, Haojie
    Shi, Chong
    Huang, Guosheng
    RSC ADVANCES, 2016, 6 (62) : S7232 - S7235
  • [22] NK1 receptor antagonists
    Lloyd, AW
    DRUG DISCOVERY TODAY, 1998, 3 (04) : 191 - 191
  • [23] Regioselective synthesis of 1,2,4-trisubstituted imidazole from a mechanistic and synthetic prospective
    Punia, Suman
    Verma, Vikas
    Kumar, Devinder
    Singh, Gurjaspreet
    Sahoo, Subash C.
    SYNTHETIC COMMUNICATIONS, 2020, 50 (05) : 700 - 709
  • [24] Biphenyl derivatives as novel dual NK1/NK2-receptor antagonists
    Mah, R
    Gerspacher, M
    von Sprecher, A
    Stutz, S
    Tschinke, V
    Anderson, GP
    Bertrand, C
    Subramanian, N
    Ball, HA
    BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2002, 12 (16) : 2065 - 2068
  • [25] Discovery of novel, orally active dual NK1/NK2 antagonists
    Bernstein, PR
    Aharony, D
    Albert, JS
    Andisik, D
    Barthlow, HG
    Bialecki, R
    Davenport, T
    Dedinas, RF
    Dembofsky, BT
    Koether, G
    Kosmider, BJ
    Kirkland, K
    Ohnmacht, CJ
    Potts, W
    Rumsey, WL
    Shen, LH
    Shenvi, A
    Sherwood, S
    Stollman, D
    Russell, K
    BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2001, 11 (20) : 2769 - 2773
  • [26] Synthesis and investigation of the biological roles of 1,4-disubstituted and 1,2,4-trisubstituted cyclohexadienes
    Benson, Jenna M.
    Bench, Bennie J.
    Watanabe, Coran M. H.
    ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 2007, 233 : 104 - 104
  • [27] Comparison of selective neurokinin receptor antagonists (NK1, NK2, NK3) and mixed profile antagonists (NK1/2, NK1/2/3) in a model of visceral hypersensitivity in rats
    Reiche, Dania
    Jasserand, Daniel
    Sann, Holger
    Preuschoff, Ulf
    Antel, Jochen
    GASTROENTEROLOGY, 2006, 130 (04) : A338 - A338
  • [28] Liquid crystals posessing 1,2,4-trisubstituted benzene derivatives
    Mahajan, R
    Nandedkar, H
    Daniel, S
    MOLECULAR CRYSTALS AND LIQUID CRYSTALS, 2001, 368 : 4465 - 4475
  • [29] Amination/annulation of chlorobutenones with chiral amine compounds:: synthesis of 1,2,4-trisubstituted pyrroles
    Demir, AS
    Igdir, AC
    Günay, NB
    TETRAHEDRON-ASYMMETRY, 2005, 16 (19) : 3170 - 3175
  • [30] APPLICATION OF LIGAND ASSISTED NUCLEOPHILIC ADDITIONS - SYNTHESIS OF 1,2,4-TRISUBSTITUTED AROMATIC SYSTEMS
    MARYANOFF, CA
    CHERRY, DA
    MILLS, JE
    PARAGAMIAN, V
    LIOTTA, D
    JAMISON, WCL
    SOLOMON, M
    ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 1987, 194 : 120 - ORGN