| abstract |
NEW MATERIAL:1-Methyl-4,5-dihydroorotyl-histidyl-proline amide expressed by formula I or an acid addition salt thereof. USE:A remedy for central nervous diseases, especially exhibiting a more powerful antagonism to a pentobarbital anesthesia than a thyrotropin-releasing-hormone (TRH), etc. and having little side effect and high safety. PREPARATION:A compound expressed by formula II (X<1> is an optionally protected imino group) or a reactive thereof is condensed with a compound expressed by formula III (X<2> is an optionally protected imino group) or a salt thereof in a solvent such as tetrahydrofuran (THF), in some cases in the presence of a deacidifying agent (example; alkali metal hydroxide, etc.), preferably at -10-10 deg.C. Thereafter the protecting group thereof is eliminated, and the resultant product is converted into its acid addition salt if desired. |