Phosphorylated morpholine acetal human neurokinin-1 receptor antagonists as water-soluble prodrugs.

@article{Hale2000PhosphorylatedMA,
  title={Phosphorylated morpholine acetal human neurokinin-1 receptor antagonists as water-soluble prodrugs.},
  author={Jeffrey John Hale and Sander Gilbert Mills and Malcolm Maccoss and C. P. Jun. Dorn and John S. Debenham and Richard J. Budhu and Robert A. Reamer and Su Er W. Huskey and Debra Luffer-Atlas and Brian Jeffrey Dean and Eileen M McGowan and William P. Feeney and Sher H Chiu and Margaret A. Cascieri and Gary G. Chicchi and Marc M Kurtz and Sharon Sadowski and Elliot M Ber and Frederick D. Tattersall and Nadia Melanie Rupniak and A. Rochelle Williams and W. Stanley Rycroft and Richard J. Hargreaves and Joseph M Metzger and Duncan Euan Macintyre},
  journal={Journal of medicinal chemistry},
  year={2000},
  volume={43 6},
  pages={
          1234-41
        }
}
The regioselective dibenzylphosphorylation of 2 followed by catalytic reduction in the presence of N-methyl-D-glucamine afforded 2-(S)-(1-(R)-(3, 5-bis(trifluoromethyl)phenyl)ethoxy)-3-(S)-(4-fluoro)phenyl-4-(5-(2- phosphoryl-3-oxo-4H,-1,2,4-triazolo)methylmorpholine, bis(N-methyl-D-glucamine) salt, 11. Incubation of 11 in rat, dog, and human plasma and in human hepatic subcellular fractions in vitro indicated that conversion to 2 would be expected to occur in vivo most readily in humans during… CONTINUE READING
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The metabolic disposition of aprepitant, a substance P receptor antagonist, in rats and dogs.

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