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Titolo:
Improved synthesis of a new nonpeptidic inhibitor of human neutrophil elastase
Autore:
Ohmoto, K; Yamamoto, T; Horiuchi, T; Kojima, T; Hachiya, K; Hashimoto, S; Kawamura, M; Nakai, H; Toda, M;
Indirizzi:
Ono Pharmaceut Co Ltd, Minase Res Inst, Osaka 6188585, Japan Ono Pharmaceut Co Ltd Osaka Japan 6188585 Res Inst, Osaka 6188585, Japan Ono Pharmaceut Co Ltd, Fukui Res Inst, Fukui, Japan Ono Pharmaceut Co LtdFukui Japan Co Ltd, Fukui Res Inst, Fukui, Japan
Titolo Testata:
SYNLETT
fascicolo: 2, , anno: 2001,
pagine: 299 - 301
SICI:
0936-5214(200102):2<299:ISOANN>2.0.ZU;2-R
Fonte:
ISI
Lingua:
ENG
Soggetto:
HUMAN-LEUKOCYTE ELASTASE; EMPHYSEMA; DESIGN;
Keywords:
enzyme inhibitor; aminopyrimidinone; ketooxadiazole; Lossen rearrangement; anionic addition reaction;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Physical, Chemical & Earth Sciences
Citazioni:
8
Recensione:
Indirizzi per estratti:
Indirizzo: Nakai, H Ono Pharmaceut Co Ltd, Minase Res Inst, Osaka 6188585, Japan Ono Pharmaceut Co Ltd Osaka Japan 6188585 Osaka 6188585, Japan
Citazione:
K. Ohmoto et al., "Improved synthesis of a new nonpeptidic inhibitor of human neutrophil elastase", SYNLETT, (2), 2001, pp. 299-301

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 nonpeptidicorally active inhibitor of human neutrophil elastase (HNE), was developed. This method includes a Losen rearrangement instead of an explosive Curtiusrearrangement and the improved preparation of the alpha -aminoketone.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 09/04/20 alle ore 12:50:43