Describes the chemical synthesis of an isotopically-labeled factor Xa inhibitor to facilitate NMR-based binding studies.
Enables REDOR NMR binding studies of factor Xa inhibitors; leaves open any clinical translation to anticoagulation.
The synthesis of an isotopically-labeled, diphenoxypyridine factor Xa inhibitor, 3-[[6-[3-(4,5-dihydro-1-(13C)-methyl-1H-(4-13C,15N2-imidazol-2-yl)phenoxy)-3,5-difluoro-4-(4-morpholinyl)-2-pyridinyl]oxy]-4-hydroxybenzene-13C-carbox-15N-imid-15N-amide, is reported for use in factor Xa binding studies using REDOR NMR. N-benzyl protected tetralabeled N-methylethylene diamine was an intermediate in the preparation of 3-[4,5-1-(13C)-methyl-1H-(4-13C,15N2-imidazol-2-yl)]phenol.
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Guilford et al. (2001) studied this question.
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