abstract |
NEW MATERIAL:A carbostyryl derivative of formula I (R<1> is H, lower alkyl, lower alkenyl, etc.; R<2> is H, OH; R<3> is H, halogen, lower alkyl, etc.; X is halogen; l, m are 0 or an interger of 1-6, provide that l+m<=6; n is 0, 1, 2; C-C bond between the 3- and 4-positions of carbostyryl skeleton is single or double bond), or its acid addition salt. EXAMPLE:5-[2-Hyroxy-3-(4-phenylpiperadinyl)propoxy]-3,4-dihydrocarbost yryl and its derivative obtained by the dehydrogenation of 3- and 4-position H atoms. USE:Antihistaminics and sedatives. PROCESS:The compound I is prepared by reacting a compound with a compound III without solvent or in an inert solvent such as dioxane, etc., in the presence of a dehydrohalogenating agent such as K2CO3, etc., and optionally a reaction accelerator such as KI, etc., at room temp. -200 deg.C, pref. 60-120 deg.C for several to 24 hours. |