| 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 wherein C n H 2n in which n is 1-7 is an alkylene radical and separates the C atom carrying the radical Py from C* by 1-3 C atoms inclusive, Py is a pyridyl residue optionally substituted by 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 heterocyclic ring) 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 their acid addition and quaternary ammonium salts are prepared by reacting a compound of the formula with a compound wherein R z is alkyl, alkoxy, tetrahydropyranyloxy, NR 3 R 4 or O-A-NR 3 R 4 and Hal is a halogen atom, in the presence of an inert organic solvent, or by dehydrating a compound of the formula or (wherein R 1 is O-A-NR 3 R 4 ) by reacting a compound I wherein R 1 is OH with a compound R 3 R 4 N-A-Hal. Starting materials include p.(2.diethylamino. ethoxy) bromobenzene from p-bromophenol and diethylaminoethyl chloride, and other aminoalkoxyhalides (including heterocyclic alkoxy halides); 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 nitrile and H 2 O 2 , together with other pyridineamides from the foregoing nitriles, and the ketones of Formula II by cyclizing the corresponding acetamides. Phormateutical compositions comprise the compounds of Formula I and a suitable carrier. The compositions, which are useful: as antifertility, anti-estrogenenic, gonadotrophin-inhibiting, blood lipid and cholesterol lowering anti-inflammatory, CNS stimulating and antifungal agents and enzyme inhibitors, may be in forms suitable for enteral and parenteral administration. |
