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The synthesis of thiolactime 4 and first studies on the syntheses of other thiolactimes with different substituted thieno[2,3-b][1,4]thiazine moieties are described as well as the syntheses of structurally modified amidines 10 - 14 with the same basic structure. The thieno[2,3-b][1,4]thiazine derivatives were prepared by reacting methyl 5-chloro-4-nitro-2-thiophencarboxylate with ethyl thioglycolate followed by reductive cyclisation to 6, which was either first saponified and then treated with Lawesson reagent to obtain thiolactame 8 or directly reacted to thiolactame 9. Reaction of 9 with various amines led to the desired products 10 - 14. which will undergo pharmacological testing on NO synthase inhibiting activities.

Synthese von einigen potentiellen NO-Synthase-Inhibitoren mit Thieno[2,3-b] [1,4l thiazin-Grundgerüst