| 摘要 |
Process for producing N-alkylated peptides with formula 1, where R1 denotes hydrogen, lower alkyl C1 to C4, carboxyl, methoxy carboxyl, ethoxy carboxyl, R2 denotes 2-phenylethylene, benzyl, A, B, C and D denote residue of natural amino acids, with exception of icysteine, involving reaction of peptide with aldehyde or ketone in the presence of a reducing agent in organic solvent medium, characterised in that N- or N-and C- preserved peptide with formula 2, where R3 denotes benzyloxycarbonyl, p-chloro, p-bromo-, p-nitro-, p-Methoxy-benzyloxycarbonyl, trityl, benzyl, p-phenylo and p-methoxy phenyl azo benzyloxycarbonyl and R denotes hydrogen, benzyl, p-nitro and p-methoxy-benzyl, are subjected to reaction with aldehyde or ketone with formula 3, where R1 and R2 have the above meaning, in the presence of water absorbing agents, preferably molecular sieves and hydrogen and palladium or ruthenium catalyst in the organic catalyst medium, optimally ethanol. The product is separated at the end of reaction using known methods.<IMAGE>
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