Due to these biological activities, the synthesis of benzothiazole is a considerable area of current discussion. The classical method involves condensation of o-aminothiophenols with substituted aldehydes 8-14, acyl chlorides, carboxylic acids 15-16 or esters, nitriles 17. Other most commonly used methods include Pd/Cu/Mn/chloranil catalyzed cyclization of o-halothioformanilides 18-22. The survey of literature related to benzothiazoles reveals the presence of this bicyclic ring system in various amine or terrestrial natural compounds, which have useful biological properties 23. Benzothiazole derivatives possess a wide spectrum of biological applications such as antitumor 26-52, antimicrobial 54-83, schictosomicidal 84, anti-inflammatory 85-93, anticonvulsants 94-102, antidiabetic 103-108, antipsychotic 109 and diuretic 111 etc.

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The synthesis of N-benzoyl-D-daunosamine - …
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A series of 3-pyridylmethyl-substituted-2-amino-6-hydroxy benzothiazoles (3.7) and 7-chloro-6-flouro-N (substituted hydrazones)-benzothiazoles (3.8) was synthesized and tested for anti-inflammatory activity. Test compound (3.7) imparted a dual inhibitory action against leukotriene B4 and thromboxane A2, which was a result of direct action on 5-lipoxygenase and TXA2 synthetase 89, 90.


Various substituted 4-(m-hydroxy-p-methoxy phenyl)-1-[(6’-flouro-7’-substituted (1, 3) - benzothiazol-2’-yl)-amido-2-phenyl]-3-chloro azetidin-2-one were synthesized and evaluated for anti-inflammatory activity. Among tested compounds (3.5) and (3.6) showed significant activity 88.

Part 3: On the synthesis of 14C-radiolabelled isopropyl-[4'-chlorobenzoyl)-2-phenoxy-2-methyl]-propionate (LF-178).
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Reaction scheme for total synthesis of the natural …

Given review is a brief account of some commonly used methods to synthesize benzothiazole derivatives and various structural alterations conducted on benzothiazole ring and preferential specificities imparted in their biological responses.

N-benzoylimido complexes of palladium

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