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The invention pertains to a combination and process for the production of 2-alkyl-4-phenyl-1,2-dihydroquinoline-3-carbonitriles and further, with very few exceptions, to all of the known corresponding substituted phenyl derivatives of the dihydroquinolines, as well as to all of the 3-carbonitriles.
For the past two decades 2-alkyl-4-phenyl-1,2-dihydroquinoline-3-carbonitriles have become known as active pharmaceutical ingredients. They belong to a class of drugs with a broad spectrum of therapeutic activity (A. Makuch, Pharmazie, 32 (1977), 75; A. Makuch, Drugs of Today, 25 (1989), 209). These organic compounds occur as natural products and are found in many plants or are obtained by the chemical synthesis (A. Makuch, Pharmazie, 32 (1977), 75; K. T. Baginsky, M. A. Mekulev, R. A. Zitenko, A. V. Zakharchenko, Chemistry and Industry, 65 (1972), 630). The most important representatives are the alkaloids humuline, ephedrine and their derivatives (C. Veenstra, Journal of Organic Chemistry, 33 (1968), 4301). Moreover, they have no secondary effects and are also well tolerated by the body.
In EP 0 759 952, 2-alkyl-4-phenyl-1,2-dihydroquinoline-3-carbonitriles are described which are produced by the reaction of 2-alkyl-4-substituted phenyl-1,2-dihydroquinolines with cyanamide. For the synthesis of these compounds the 2-alkyl-4-substituted phenyl-1,2-dihydroquinolines are first of all synthesized from an appropriate 2-alkylpyridine and the appropriate 2-alkyl-4-substituted phenyl-1,2-dihydroquinoline is then prepared from this 2-alkylpyridine by reaction with an amine. The 2-alkyl-4-substituted phenyl-1,2-dihydroquinolines can be synthesized by reaction of the appropriate 2-alkylpyridine with phen
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