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Synlett 1996; 1996(4): 359-360
DOI: 10.1055/s-1996-5420
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Synthesis of 5-N-Substituted Tetrazole Derivatives of the Potent NK1 Receptor Antagonist GR203040

Miles S. Congreve*
  • *Glaxo Wellcome Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire, SG1 2NY
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Publikationsdatum:
31. Dezember 2000 (online)

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A series of amino-tetrazole derivatives of GR203040 were synthesised as potential NK1 receptor antagonists. The synthesis of these analogues utilised a novel reaction sequence in which 1-aryl tetrazoles were converted to 1-aryl-5-amino-tetrazoles via a cyanoamide intermediate.

neurokinin-1-receptor antagonist - aminotetrazole - cyanoamide