Acylation of amino acids

C - Chemistry – Metallurgy – 07 – D

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530/5.06, 260/46

C07D 207/46 (2006.01) C07D 207/404 (2006.01)

Patent

CA 1084908

TITLE ACYLATION OF AMINO ACIDS INVENTOR Alenka. M. Paquet ABSTRACT OF THE DISCLOSURE N-monosubstituted derivatives of diamino acids are prepared by the reaction of succinimidyl esters of car- boxylic acids or substituted carbonic acids with the, un- protected diamino acid. The acylation preferentially occurs at the side chain or terminal amino group of the diamino acid. For example, selective acylation of the terminal amino group of lysine occurs without first having protected the 2-amino group. Such acylation has application in the preparation of inter alia N6-palmitoyl-lysine. A novel advantageous route for preparing the succinimidyl esters is also described.

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