Process Development of (2-Nitrophenylcarbamoyl)-(S)-prolyl-(S)-3-(2-naphthyl) alanyl-N-benzyl-N-methylamide (SDZ NKT343)

…, O Repic, TJ Blacklock, W Prikoszovich

文献索引：Prashad, Mahavir; Prasad, Kapa; Repic, Oljan; Blacklock, Thomas J.; Prikoszovich, Walter Organic Process Research and Development, 1999 , vol. 3, # 6 p. 409 - 415

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被引用次数: 8

摘要

(2-Nitrophenylcarbamoyl)-(S)-prolyl-(S)-3-(2-naphthyl) alanyl-N-benzyl-N-methylamide (1; SDZ NKT343) is a human NK-1 tachykinin receptor antagonist. The development of a robust process for a multikilogram scale, chromatography-free preparation of this compound is described. The new four-step synthesis was based on a convergent approach, which utilized a peptide coupling of 1-[(2-nitrophenylamino) carbonyl]-l-proline (11) with free base of (S)- ...