Abstract
The reaction of the tetrahydrobenzo[b]thiophene derivatives 1a,b with benzoylisothiocyanate (2) afforded the thiourea derivatives 3a,b. Cyclization of the latter products gave the annulated products 4a,b. Compounds 3a,b reacted with either hydrazine hydrate (5a) or phenyl hydrazine (5b) afforded compounds 7a-d which underwent cyclization for compounds 7a,c afforded compound 9. On the other hand compounds 4a,b reacted with either hydrazine hydrate (5a) or phenyl hydrazine (5b) afforded compounds 6a-d a second pathway was applied to synthesize compound 6c which underwent cyclization afforded compound 9. Also compounds 4a,b reacted with either phenacyl bromide (10) afforded compounds 11a,b or ethylchloroacetae (12) compounds 13a,b were produced. The latter products reacted with each hydrazine hydrate (5a) and phenyl hydrazine (5b) afforded compounds 14a-d. Their antitumor activities were tested using three different cell lines.
Highlights
Over the past few years some research groups and our group were interested to introduce a comprehensive study program towards the synthesis of thiophenes and their fused derivatives [1,2,3,4]
Compounds 4a,b reacted with either phenacyl bromide (10) afforded compounds 11a,b or ethylchloroacetae (12) compounds 13a,b were produced. The latter products reacted with each hydrazine hydrate (5a) and phenyl hydrazine (5b) afforded compounds 14a-d
The importance of such compounds based on their uses as anti-inflammatory [5,6,7] thiophene derivatives was evaluated as antiprotozoal [8,9], on the other hand thiophene derivatives was applied as a new antitumor agents [10,11], in addition to fused thiophene derivatives was tested as templates for serine protease inhibition [12] and alternate substrate inhibitors of cholesterol esterase [13]
Summary
Over the past few years some research groups and our group were interested to introduce a comprehensive study program towards the synthesis of thiophenes and their fused derivatives [1,2,3,4]. The importance of such compounds based on their uses as anti-inflammatory [5,6,7] thiophene derivatives was evaluated as antiprotozoal [8,9], on the other hand thiophene derivatives was applied as a new antitumor agents [10,11], in addition to fused thiophene derivatives was tested as templates for serine protease inhibition [12] and alternate substrate inhibitors of cholesterol esterase [13]. In this article we are using the 2-amino-4,5,6,7-tetrahydrobenzo[b] thiophene derivatives [14] 1a,b in the synthesis of fused derivatives of pharmaceutical interest
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