| 摘要 |
<p>1,188,505. N,N<SP>1</SP>-Disubstituted piperazines. H. E. SAUNDERS. 27 June, 1967 [27 June, 1966], No. 28801/66. Heading C2C. Novel compounds of formula (wherein R is C 1-6 alkyl, and R 1 , R 2 and R 3 are each hydrogen, halogen, alkyl, alkoxy, alkenyloxy or 2-aminoalkoxy) are prepared by reacting styrene with tertiary-butyl hypobromite and an alkanol of formula ROH (wherein R is as defined above), reacting the resulting 2-phenyl-2-alkoxyethyl bromide with piperazine, subjecting the resulting 1 - (2 - phenyl - 2 - alkoxy - ethyl) - piperazine to a Mannich reaction with formaldehyde (or trioxymethylene) and acetophenone bearing substituents corresponding to R 1 , R 2 and R 3 , and lastly reducing the resulting 1 - [2 - phenyl - 2 - alkoxy - ethyl] - 4 - [2 - (optionally substituted) benzoyl-ethyl]-piperazine with sodium borohydride. The compounds of Formula I possess bronchial spasmolytic activity and may be incorporated with suitable excipients into pharmaceutical compositions suitable for administration in the forms of injectable ampoules, tablets, suppositories and aerosols. Reference has been directed by the Comptroller to Specifications 1,097,572 and 1,119,835.</p> |
