Novel synthesis of 5,11-dihydro-6H-pyrido[2,3-b]-[1,4]benzodiazepin-6-ones and related studies |
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Authors: | M. Oklobd ija,G. Comisso,E. Decorte,T. Fajdiga,G. Gratton,F. Moimas,R. Toso,V. unji |
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Affiliation: | M. Oklobdžija,G. Comisso,E. Decorte,T. Fajdiga,G. Gratton,F. Moimas,R. Toso,V. Šunjić |
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Abstract: | 5,11-Dihydro-6H-pyrido[2,3-6][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 compound 20 , and return of the latter into 5 is described. |
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