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Non‐peptide fibrinogen receptor antagonists. 3 1 . The synthesis of [ 3 H]L‐767,685 and [ 3 H]L‐767,679
Author(s) -
Hamill Terence G.,
Hutchinson John H.,
Hartman George D.,
Burns H. Donald
Publication year - 1998
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/(sici)1099-1344(199807)41:7<677::aid-jlcr118>3.0.co;2-l
Subject(s) - chemistry , prodrug , halogenation , hydrolysis , peptide , tritium , receptor , catalysis , specific activity , stereochemistry , antagonist , peptide synthesis , chemical synthesis , fibrinogen , tritium illumination , organic chemistry , biochemistry , enzyme , in vitro , physics , nuclear physics
The synthesis of the fibrinogen receptor antagonist [ 3 H]L‐767,679 and its ethyl ester prodrug [ 3 H]L‐767,685 is described. Bromination of an appropriate benzolactam followed by catalytic tritiation with tritium gas gave a labelled benzolactam that was converted to [ 3 H]L‐767,685 via a coupling/deprotection sequence. Hydrolysis of [ 3 H]L‐767,685 then gave the acid [ 3 H]L‐767,679. These two compounds were obtained with a specific activity of 10–16 Ci/mmol. © 1998 John Wiley & Sons, Ltd.