| 摘要 |
NEW MATERIAL:A compound shown by the formula I (R<1> is H, lower alkenyl, lower alkynyl, etc.; R<2> is H, lower alkyl, or phenyl; R<3> is phenyl or lower alkyl having phenyl as a substituent; X is halogen; Y is lower alkylene; n is 0-2; dotted line is single or double bond). EXAMPLE:5-[2-Hydroxy-3-(4-phenylpiperidinyl)propoxy]-3,4-dihydrocarbos tyril. USE:An antihistaminic having antihistaminic action and inhibition of central nervous system. PROCESS:A compound shown by the formula II (X<1> is halogen) is reacted with a piperidine derivative shown by the formula III in the absence of a solvent or in an inert solvent (e.g., dioxane, THF, etc.) at room temperature to 200 deg.C, preferably 60-120 deg.C, to give a compound shown by the formula I. The compound shown by the formula II as a starting material is obtained by reacting a compound shown by the formula IV with a compound shown by the formula V (X<2> is halogen). |
