Collect. Czech. Chem. Commun. 1994, 59, 667-674

Antihistamine Substances. Tricyclic Analogues of N-(4,4-Diphenyl-3-butene-1-yl)nipecotic Acid and Some Related Compounds

Karel Šindelářa, Alexandra Šilhánkováa, Jiří Urbanb, Jan Metyša, Martin Valchářa and Zdeněk Polívkaa

a Research Institute for Pharmacy and Biochemistry, 130 00 Prague 3, Czech Republic
b J. Heyrovský Institute of Physical Chemistry, Academy of Sciences of the Czech Republic, 182 23 Prague 8, Czech Republic


Alkylation of ethyl nipecotate with bromides VII - X gave amino esters Ib - Vb. Alkylation of ethyl piperazine-2-carboxylate with 4-bromo-1,1-diphenyl-1-butene afforded compound Vb. Final product Ia - Va were obtained by acid hydrolysis of corresponding esters Ib - Vb. Some of the compounds showed significant antihistamine and antiulcer activities.