Thiophene systems. 7. Pyrido[3,2-b]thieno[3,4-e][1,4]diazepine derivatives with potential cns activity |
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Authors: | Jeffery B Press Corris M Hofmann Gretchen E Wiegand Sidney R Safir |
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Abstract: | Pyrido3,2-b]thieno3,4-e]1,4]diazepines ( 1a-d ) were synthesized to investigate their potential CNS activity. Synthesis of the desired ring system was effected by condensation of 2,3-diaminopyridine ( 3 ) with methyl tetrahydro-4-oxo-3-thiophenecarboxylate ( 4 ). Structural assignment of the major condensation product 5 was determined by comparison of 1H nmr absorptions of 5 with those of related methyl lactam derivatives 11 and 14. A discussion of the possible mechanism leading to 5 in preference to isomeric lactam 6 is presented. Biological evaluation of 1a-d revealed no interesting properties. |
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