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Synthesis of [ O ‐methyl‐ 11 C]‐4‐(1,3‐dimethoxy‐2‐propylamino)‐2,7‐dimethyl‐8‐(2,4‐dichlorophenyl)[1,5‐a]pyrazolo‐1,3,5‐triazine ([ 11 C]DMP696): a potential PET ligand for CRF 1 receptors
Author(s) -
Kumar J. S. Dileep,
Majo Vattoly J.,
Simpson Norman R.,
Prabhakaran Jaya,
Van Heertum Ronald L.,
Mann J. John
Publication year - 2004
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/jlcr.885
Subject(s) - chemistry , trifluoromethanesulfonate , yield (engineering) , triazine , chemical synthesis , medicinal chemistry , d 1 , stereochemistry , organic chemistry , receptor , catalysis , in vitro , biochemistry , materials science , metallurgy
Synthesis of [ O ‐methyl‐ 11 C]‐4‐(1,3‐dimethoxy‐2‐propylamino)‐2,7‐dimethyl‐8‐(2,4‐dichlorophenyl)[1,5‐a]pyrazolo‐1,3,5‐triazine ([ 11 C]DMP696), a highly selective CRF 1 antagonist has been achieved. The total time required for the synthesis of [ 11 C]DMP696 is 30 min from EOB using [ 11 C]methyl triflate in THF, with a 16% yield (EOS) and >99% chemical and radiochemical purities along with a specific activity of >2000 Ci/mmol (EOS). Copyright © 2004 John Wiley & Sons, Ltd.

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