Synlett

Improved Synthesis of a New Nonpeptidic Inhibitor of Human Neutrophil Elastase

…, T Kojima, K Hachiya, S Hashimoto, M Kawamura…

Index: Ohmoto; Yamamoto; Horiuchi; Kojima; Hachiya; Hashimoto; Kawamura; Nakai; Toda Synlett, 2001 , # 2 p. 299 - 301

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Citation Number: 8

Abstract

Abstract: A practical method for the synthesis of ONO-6818 {2-(5-Amino-6-oxo-2- phenylhydropyrimidinyl)-N-[2-(5-tert-butyl-1, 3, 4-oxadiazol-2-yl)-1-(methylethyl)-2-oxoethyl] acetamide}(1), the first clinical candidate for a nonpeptidic orally active inhibitor of human neutrophil elastase (HNE), was developed. This method includes a Lossen rearrangement instead of an explosive Curtius rearrangement and the improved preparation of the a- ...