Search

By the addition of equivalent amount of appropriate amine on the carbon-carbon double bond of N-substituted maleamic acids under the influence of pyridine, a number of potential hypocholesteremics, N,N2-disubstituted DL-β-asparagines was prepared. For all N-alkyl- and N-arylmaleamic acids, the addition proceeded smoothly and resulted in satisfactory yields, but in the cases of N-heterocyclic analogs, transamidation was observed to occur simultaneously with the addition reactions.

In a search for substances that might be useful hypocholesteremic agents, a series of twenty five N-substituted maleamic acids was prepared. These compounds were produced in satisfactory yields by the aminolysis of maleic anhydride with appropriate aliphatic, aromatic and heterocyclic amines in various solvents under similar conditions. Analytical data as well as spectroscopic characterizations are provided.