Describes the chemical synthesis of an isotopically-labeled factor Xa inhibitor for use in NMR binding studies.
Facilitates NMR binding studies of factor Xa inhibitors; leaves open any clinical translation.
The synthesis of an isotopically‐labeled, diphenoxypyridine factor Xa inhibitor, 3‐[[6‐[3‐(4,5‐dihydro‐1‐( 13 C)‐ methyl ‐1 H ‐(4‐ 13 C, 15 N 2 ‐ imidazol ‐2‐yl)phenoxy)‐3,5‐difluoro‐4‐(4‐morpholinyl)‐2‐pyridinyl]oxy]‐4‐hydroxybenzene‐ 13 C‐ carbox ‐ 15 N‐ imid ‐ 15 N‐ 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‐( 13 C)‐ methyl ‐1 H ‐(4‐ 13 C, 15 N 2 ‐ imidazol ‐2‐yl)]phenol.
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Guilford et al. (2001) studied this question.
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