Non-peptide fibrinogen receptor antagonists.: 4.: The synthesis of [3H]L-756,568.

被引:0
|
作者
Hamill, TG
Hutchinson, JH
Brashear, KM
Hartman, GD
机构
[1] Merck Res Labs, Dept Pharmacol, W Point, PA 19486 USA
[2] Merck Res Labs, Dept Med Chem, W Point, PA 19486 USA
关键词
fibrinogen receptor antagonist; L-756,568; catalytic tritiation;
D O I
10.1002/(SICI)1099-1344(199906)42:6<605::AID-JLCR222>3.0.CO;2-L
中图分类号
Q5 [生物化学];
学科分类号
071010 ; 081704 ;
摘要
The synthesis of [H-3]L-756,568, an orally active fibrinogen receptor antagonist, is described. Two synthetic pathways were developed using either bromoindoles 2a/2b or bromoaryl sulfonamide 11 as the precursor. Use of the bromoaryl sulfonamide precursor led to [H-3]L-756,568 with higher radiochemical purity, higher radiochemical yield, and slightly higher specific activity.
引用
收藏
页码:605 / 609
页数:5
相关论文
共 50 条
  • [1] Non-peptide fibrinogen receptor antagonists. 4. The synthesis of [3H]L-756,568
    Hamill, Terence G.
    Hutchinson, John H.
    Brashear, Karen M.
    Hartman, George D.
    Journal of Labelled Compounds and Radiopharmaceuticals, 1999, 42 (06): : 605 - 609
  • [2] Non-peptide fibrinogen receptor antagonists. 2. The synthesis of [3H]L- 738,167
    Merck Research Laboratories, Department of Pharmacology, WP44C-2, West Point, PA 19486, United States
    不详
    J. Label. Compd. Radiopharm., 4 (273-277):
  • [3] Non-peptide fibrinogen receptor antagonists.: 3.: The synthesis of [3H]L-767,685 and [3H]L-767,679.
    Hamill, TG
    Hutchinson, JH
    Hartman, GD
    Burns, HD
    JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS, 1998, 41 (07): : 677 - 680
  • [4] Non-peptide fibrinogen receptor antagonists. 3. The synthesis of [3H]L- 767,685 and [3H]L-767,679
    Merck Research Laboratories, Department of Pharmacology, West Point, PA 19486, United States
    不详
    J. Label. Compd. Radiopharm., 7 (677-680):
  • [5] Non peptide fibrinogen receptor antagonists.: 2.: The synthesis of[3H]L-738,167.
    Hamill, TG
    Askew, BC
    Hartman, GD
    Claremon, DA
    McIntyre, CJ
    Burns, HD
    JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS, 1998, 41 (04): : 273 - 277
  • [6] Discovery of potent, non-peptide thrombin receptor antagonists.
    Chackalamannil, S
    Xia, Y
    Clasby, M
    Greenlee, W
    Doller, D
    Eagen, K
    Tsai, HS
    Asberom, T
    Lin, Y
    Czarniecki, M
    Ahn, HS
    Foster, C
    Boykow, G
    ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 2001, 221 : U60 - U60
  • [7] Non-peptide calcitonin gene-related peptide (CGRP) receptor antagonists.
    Daines, RA
    Sham, KKC
    Taggart, JJ
    Kingsbury, WD
    Chan, J
    Breen, A
    Disa, J
    Aiyar, N
    ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 1997, 214 : 237 - MEDI
  • [8] Synthesis and SAR studies with a first in class series of non-peptide motilin receptor antagonists.
    Xiang, MA
    Ryhczynski, P
    Chen, RHK
    Beavers, MP
    Combs, DW
    Gunnet, JI
    Hageman, W
    Moore, JB
    Zhou, LB
    Urbanski, M
    Demarest, KT
    ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 2004, 228 : U912 - U912
  • [9] Design and synthesis of amidino-tyrosine derivatives as non-peptide fibrinogen receptor antagonists
    Xu, TL
    Jiang, XT
    Hua, WY
    Ni, PZ
    Pei, YM
    BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 1999, 9 (14) : 1933 - 1936
  • [10] Design, synthesis, and activity of a new class of chain-shortened non-peptide αvβ3 receptor antagonists.
    Coleman, P
    Askew, BC
    Brashear, KM
    Duggan, ME
    Halczenko, W
    Hartman, GH
    Hutchinson, JH
    Hunt, CA
    Meissner, RS
    Perkins, JJ
    Whitman, D
    Duong, LT
    Leu, CT
    Nagy, RM
    Rodan, GA
    Rodan, SB
    Fernandez-Metzler, C
    Merkle, K
    Preksaritanont, T
    Lynch, JL
    Stump, G
    Wallace, A
    ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 2001, 222 : U671 - U671