VITAMIN E DERIVATIVE AND ANTIULCER AGENT CONTAINING THE SAME AS ACTIVE INGERDIENT

摘要

PURPOSE: To obtain a new compound having excellent antiulcer action, useful as an antiulcer agent and capable of continuously using for a long period because of extremely reduced toxicity and side effects. ;CONSTITUTION: A vitamin E derivative of formula I (X is H or acyl) or its salt. The compound is obtained by reacting, e.g. carnosine of formula II with a compound of the formula Z-Cl (Z is amino acid protecting group) in an alkaline solution of NaOH aqueous solution at pH 8-10 and -10 to 10°C to afford carnosine having a protected amino group and reacting the resultant compound with tocopherol of formula III in the presence of a dehydration condensing agent such as thionyl chloride in a solvent such as THF at -10-30°C to afford a vitamin E derivative having protected amino group and expressed by formula IV and hydrogenating the compound of formula IV at 15-50°C in the presence of a catalyst such as Pd-carbon in an inert solvent.;COPYRIGHT: (C)1994,JPO&Japio