Synthesis of a Novel Dual Inhibitor of Thromboxane A2 Synthetase and 5-Lipoxygenase (E3040) via the Direct Coupling Reaction of Hydroquinone with 3-Pyridinecarboealdehyde

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, wa...

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Bibliographic Details
Published inChemical & pharmaceutical bulletin Vol. 43; no. 10; pp. 1614 - 1616
Main Authors KOMATSU, Yuki, MINAMI, Norio
Format Journal Article
LanguageEnglish
Published Tokyo The Pharmaceutical Society of Japan 15.10.1995
Japan Science and Technology Agency
Subjects
2, 6-dimethyl-1, 4-benzohydroquinone
5-lipoxygenase
direct coupling reaction
dual inhibitor
pyridinecarboxaldehyde
thromboxane A2 synthetase
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Summary: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 6N hydrochloric acid. The regio isomers of 3-pyridinecarboxaldehyde also gave the corresponding coupling products in high yields.
ISSN:0009-2363
1347-5223
DOI:10.1248/cpb.43.1614