发明名称 |
SOLID PHASE AND COMBINATORIAL SYNTHESIS OF SUBSTITUTED 2-METHYLENE-2,3-DIHYDROTHIAZOLES AND OF ARRAYS OF SUBSTITUTED 2-METHYLENE-2,3-DIHYDROTHIAZOLES |
摘要 |
A solid phase method for the synthesis of a plurality of differently substituted 2-methylenethiazoles with a wide variety of side-chain substituents as compounds of potential therapeutic interest. The 2-methylenethiazoles are prepared by acylation of a substrate-bound primary or secondary amine with cyanoacetic acid and reaction of the resulting cyanoacetamide with an isothiocyanate in the presence of a base. Alkylation with an appropriate alkyl halide under acidic conditions yields differently substituted, support-bound 2-methylene-2,3-dihydrothiazoles. These may be screened on the substrate or cleaved from the substrate and then screened in solution. The efficient synthesis of a wide variety of 2-methylenethiazoles using automated synthesis technology of the present method makes these compounds attractive candidates for the generation and rapid screening of diverse thiazole-based libraries. The method disclosed here provides an easy and fast access to highly diverse heterocyclic compounds of therapeutic interest, amenable to automatization.
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申请公布号 |
WO9740030(A1) |
申请公布日期 |
1997.10.30 |
申请号 |
WO1997DK00187 |
申请日期 |
1997.04.24 |
申请人 |
NOVO NORDISK A/S;DOERWALD, FLORENCIO, ZARAGOZA |
发明人 |
DOERWALD, FLORENCIO, ZARAGOZA |
分类号 |
C07D277/14;C07D277/30;(IPC1-7):C07D277/30;A61K31/41 |
主分类号 |
C07D277/14 |
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