1-AND/OR 3-SUBSTITUTED-4-OXO-2-AZETIDINYLCARBONYL DERIVATIVE AND PREPARATION THEREOF

• Main Authors: TAMURA TOSHIYA, KAGAMI SOUICHI, IWAMOTO HIDENORI, YAMAMOTO MINORU, YOSHIDA MAKOTO
• Format: Patent
• Language: English
• Published: 18.01.1986
• Subjects: ACYCLIC OR CARBOCYCLIC COMPOUNDS; CHEMISTRY; HETEROCYCLIC COMPOUNDS; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS

NEW MATERIAL:A compound expressed by formula I [R is H or substituted lower alkyl; R is H or (substituted) lower alkyl; R is expressed by formula IIor III (R is H or lower alkyl), provided that R and R are not H at the same time]. EXAMPLE:N-[ ( 2S,3R ) -3-Benzyl-4-oxo-2-azetidinylcarbonyl ]-L-histidyl-L-prolinamide. USE:A drug for central nervous systems useful as an ameliorant of dysbulia, e.g. schizophrenia, melancholia, sequela of cerebrovascular disorder, senile dementia, epilepsy, etc. or ameliorant of hypobulia, depression or hypomnesia, etc. PREPARATION:A 1- or 3-substituted-4-oxo-2-azetidinecarboxylic acid expressed by formula IV or both are subjected to peptide reaction with an amine expressed by formula V in an inert solvent, e.g. dimethylformamide, at room temperature under heating, and if necessary the protecting groups are removed to afford the aimed compound expressed by formula I.