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METHOD FOR THE PREPARATION OF A MEDICINAL PRODUCT WITH SOURCE CHODILATOR ACTIVITY OBTAINED FROM MEDICINAL PRODUCT OBTAINED BY THIS METHOD AND METHOD FOR PREPARING MEDICINAL COMPOUNDS FOR USE THEREOF
METHOD FOR THE PREPARATION OF A MEDICINAL PRODUCT WITH SOURCE CHODILATOR ACTIVITY OBTAINED FROM MEDICINAL PRODUCT OBTAINED BY THIS METHOD AND METHOD FOR PREPARING MEDICINAL COMPOUNDS FOR USE THEREOF
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机译:从该方法获得的医药产品中获得具有源氯化器活性的医药产品的方法及其制备药物的方法
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1316424 - Hydroxyphenyl - - (2 - piperidyl)- methanols MINNESOTA 3M LABORATORIES Ltd 19 May 1970 [20 May 1969] 25634/69 Heading C2C Novel - hydroxyphenyl - - (2 - piperidyl)- methanols of the general formula wherein R is a hydrogen atom or alkyl group; RSP1/SP is a hydrogen atom or a hydroxy or C 1-6 alkoxy group; and RSP2/SP is a hydrogen atom or an alkyl, phenyl, phenyl-alkyl, diphenyl-alkyl, phenoxy - alkyl or diphenoxy - alkyl group ("alkyl" meaning C 1-6 alkyl or C 3-6 cycloalkyl in these definitions); and pharmaceutically acceptable acid addition and quaternary ammonium salts thereof are prepared (a) by hydrogenating in the presence of a catalyst a compound of the general formula wherein B is CO or CHOH. Polyhydroxyphenyl 2-pyridyl ketones of the second general formula above wherein B is CO and RSP2/SP is a hydrogen atom or alkyl group are prepared by condensing a poly-C 1-6 alkoxybenzaldehyde with a picolinic acid, oxidizing the resulting -(poly-C 1-6 alkoxyphenyl)--(2- pyridyl)-methanol and dealkylating the resulting poly-C 1-6 alkylphenyl 2-pyridyl ketone. - (C 1-6 alkoxy - p - hydroxyphenyl) - - (2-pyridyl)-methanols of the second general formula above wherein B is CHOH and RSP2/SP is a hydrogen atom or alkyl group are prepared by treating a C 1-6 alkoxy-p-benzyloxybenzaldehyde with a 2-pyridyllithium and hydrogenating the resulting - (C 1-6 alkoxy - p - benzyloxy - phenyl)- - (2 - pyridyl) - methanol. They may be oxidized to give the corresponding ketones (B is CO). Polyhydroxyphenyl 2 - pyridyl ketones of the second general formula above wherein B is CO and RSP2/SP is a phenethyl or dibenzylmethyl group are prepared by condensing a poly-C 1-6 alkoxy-phenyl methyl-2-pyridyl ketone and 1,3- propanediol in the presence of p-toluenesulphonic acid, treating the resulting 2-(poly- C 1-6 alkoxy - phenol) - 2 - (methyl - 2 - pyridyl)- 1,3-dioxane with phenyllithium and then benzyl chloride and treating the resulting mixture of a 2 - (poly - C 1-6 alkoxy - phenyl) - 2 - (phenethyl- 2 - pyridyl) - 1,3 - dioxane and a 2 - (poly- C 1-6 alkoxy - phenyl) - 2 - (dibenzylmethyl - 2- pyridyl)-1,3-dioxane with HBr. Pharmaceutical compositions having bronchodilatory activity comprise, as active ingredient, an - hydroxy - phenyl - - (2 - piperidyl)- methanol of the first general formula above or a pharmaceutically acceptable acid addition or quaternary ammonium salt thereof, together with a pharmaceutical diluent or carrier.
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