| 摘要 |
The invention relates to beta -alanine amides of general formula (I), wherein: R<1> represents hydrogen or C1-6 alkyl that is optionally substituted by hydroxy, amino, carboxy, carbamoyl, methylmercapto, guanidino, optionally substituted aryl or heteroaryl, and; R<2> represents hydrogen or R<1> and R<2>, together, form a group of formula -(CH2)n-, wherein n is 3 or 4. Said beta -alanine amides are produced without using an amino protective group by reacting the corresponding amine with a cyanoacetic ester in order to form an acetamide and by effecting a subsequent catalytic hydrogenation. The method is suited, in particular, for producing carcinine ( beta -alanyl-histamine, R<1 >= imidazol-4-ylmethyl, R<2> = H), a naturally occurring pseudo dipeptide, which is used as an active ingredient having an antioxidative effect in medicaments and cosmetics. |
