Synthesis of a novel dual inhibitor of thromboxane A2 synthetase and 5- lipoxygenase (E3040) via the direct coupling reaction of hydroquinone with 3- pyridinecarboxaldehyde

Article abstract of DOI:10.1248/cpb.43.1614

Synthesis of a novel dual inhibitor of thromboxane A₂ synthetase and 5- lipoxygenase, 5,7-dimethyl-6-hydroxy-2-methylamino-4-(3- pyridylmethyl)benzothiazole (E3040), was accomplished via a new coupling reaction, in which a key intermediate, (3,6-dihydroxy-2,4-dimethylphenyl)- (3-pyridyl)methanol, was easily synthesized in a high yield from 2,6- dimethyl-1,4-benzohydroquinone and 3-pyridinecarboxaldehyde in 6 N hydrochloric acid. The regio isomers of 3-pyridinecarboxaldehyde also gave the corresponding coupling products in high yields.

Full text of DOI:10.1248/cpb.43.1614

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