Substituted 5-hydroxy-2,3-dihydrobenzothiophenes as inhibitors o

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

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549 51, A61K 3138, C07D33354

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049635808

ABSTRACT:
Position-4 and/or position-6 substituted 5-hydroxy-2,3-dihydrobenzothiophenes and analogs of the following general structural formula (I) are disclosed: ##STR1## These compounds are found to be potent inhibitors of leukotriene biosynthesis.

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Bordwell, F. G. and Stang, H., Benzothiophene Chemistry, VII., Substitution Reactions of 5-Hydroxy and 5-Aminobenobenzothiophene Derivatives, J. Amer. Chem. Soc., vol. 77, pp. 5939-5944, (Nov. 1955).
Feiser, L. F. and Kennelly, R. G., A Comparison of Heterocyclic Systems with Benzene, IV, Thionaphthenequinones, J. Amer. Chem. Soc., vol. 57, pp. 1611-1614, (Sep. 1935).
Fries, K.; Heering, H.; Hemmacke, K., and Siebert, G., Untersuchungen in der Reihe des Thionaphtens, Ann., vol. 527, pp. 83-113, (1936).
Oikawa, Y., and Yonemitsu, O., A New Synthesis Method for Condensed Heterocycles, Carbazoles, Indoles, and Benzothiophenes, Based on Catalyzed Cyclization of Q-Keto Sulfoxides, J. Org. Chem., vol. 41, pp. 1118-1124 (1976).
Kursanov, D. N.; Parnes, Z. N.; Loim, N. M., Application of Ionic Hydrogenation to Organic Synthesis, pp. 633-651, (Sep. 1974).

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