| 摘要 |
PROBLEM TO BE SOLVED: To obtain an optically active N,N'-ethylene-bis-α-amino acid derivative at a high yield by reacting an α-amino acid derivative with glyoxal and a reductant. SOLUTION: A compound of formula III is obtained by reacting the compounds of formulae I and II [R<1> and R<2> are each a residue of α-amino acid (excepting glycine, proline and hydroxyproline); R<11> and R<21> are each H or a carboxy protecting group; R<12> and R<22> are each H; or, R<1> and R<12> bind to form a proline ring or a hydroxyproline ring; etc.] with glyoxal and a reductant (e.g. sodium boron cyanohydride) at from -20 deg.C to 60 deg.C. The compound of formula III is an optically active substance and liposoluble, and useful as a reagent of various organic synthetic reactions, especially effective for asymmetric reactions. The compound is also useful as a ligand of an optically active metal complex, as a constitution unit of a macrocyclic compound, and further as an antibiotic, etc. |
