1-phenyl-2-pyridylbenzocycloalkenes and derivative

专利名称：1-phenyl-2-pyridylbenzocycloalkenes and

derivatives thereof

发明人：LEDNICER DANIEL,BABCOCK JOHN C.申请号：US28400863申请日：19630529公开号：US3403162A公开日：19680924

摘要：1,053,312. 1 -Phenyl.-2-pyridylbenzocycloalkenes. UPJOHN CO. April 15, 1964[May 29, 1963], No. 15635/64. Heading C2C. Compounds of the general formula whereinC n H 2n in which n is 1-7 is an alkylene radical and separates the C atom carrying theradical Py from C* by 1-3 C atoms inclusive, Py is a pyridyl residue optionally substitutedby at least one alkyl or alkoxy group or halogen atom R 1 is alkyl, alkoxy, OH, NR 3 R 4(where R 3 and R 4 are alkyl or are linked together to form a 5-7 membered heterocyclicring) or wherein A is a C 2-6 alkylene radical, R 2 is alkyl, alkenyl, CF 3 , alkoxy alkenyloxy,alkylenedioxy, cycloalkoxy, halo, alkylmercapto or NR 3 R 4 and x and y are 1-4 and theiracid addition and quaternary ammonium salts are prepared by reacting a compound ofthe formula with a compound wherein R z is alkyl, alkoxy, tetrahydropyranyloxy, NR 3 R 4or O-A-NR 3 R 4 and Hal is a halogen atom, in the presence of an inert organic solvent, orby dehydrating a compound of the formula or (wherein R 1 is O-A-NR 3 R 4 ) by reacting acompound I wherein R 1 is OH with a compound R 3 R 4 N-A-Hal. Starting materialsinclude p.(2.diethylamino. ethoxy) bromobenzene from p-bromophenol and

diethylaminoethyl chloride, and other aminoalkoxyhalides (including heterocyclic alkoxyhalides); α - (m - methoxyphenyl ethyl) - 3- pyridylacetonitrile from 3 -

pyridineacetonitrile and m - methoxy - # - phenylethyl bromide, and α - (m -methoryphenylethyl) - 2 - and 4-pyridine- and -2-, -3- and -4- alkyl-, alkoxy-, and halo -pyridine - acetonitriles; α - (mmethoxyphenylethyl)- 3 . pyridineacetamide from the nitrileand H 2 O 2 , together with other pyridineamides from the foregoing nitriles, and theketones of Formula II by cyclizing the corresponding acetamides. Phormateuticalcompositions comprise the compounds of Formula I and a suitable carrier. Thecompositions, which are useful: as antifertility, anti-estrogenenic, gonadotrophin-inhibiting, blood lipid and cholesterol lowering anti-inflammatory, CNS stimulating andantifungal agents and enzyme inhibitors, may be in forms suitable for enteral andparenteral administration.

申请人：THE UPJOHN COMPANY

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