- Novel synthesis of 5,11-dihydro-6H-pyrido[2,3-b]-[1,4]-benzodiazepin-6-ones and related studies (1)
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5,11-Dihydro-6H-pyrido[2,3-b][1,4]benzodiazepin-6-one (1), a basic intermediate in the preparation of 11-α-aminoacetyl derivatives with important biological activities, has been obtained by a three-step synthesis starting from easily available isatoic anhydride and anhydro ornithine. Some model cyclisation reactions leading to 5-member ring derivatives 10 and 12 instead of 7-member ring analogues of 1, are reported. Easy transformations of the tetrahydro congener of 1, i.e. compound 4 into 19, which actually represents a tetrahedral intermediate in the transformation of 5 into 4, is noticed. Further rearrangement of 19 into spiro compounds 20, and return of the latter into 5 is described.
- Oklobdzija,Comisso,Decorte,et al.
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p. 1329 - 1334
(2007/10/02)
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- Anti-inflammatory oxazole[4,5-b]pyridines
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The various isomers of oxazolo- and thiazolopyridines having utility as antiinflammatory, antipyretic and analgesic agents are prepared by condensation of an appropriate amino-hydroxypyridine or amino-mercaptopyridine with a carboxylic acid, halide or anhydride.
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