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Formation of N-protected bis-3,6-(4-aminoalkyl)-2,5,diketopiperazine

  • US 8,912,328 B2
  • Filed: 02/07/2012
  • Issued: 12/16/2014
  • Est. Priority Date: 02/10/2011
  • Status: Active Grant
First Claim
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1. A method for the synthesis of 3,6-bis-4-(N-trifluoroacetyl)aminobutyl-2,5- diketopiperazine comprising:

  • heating a mixture of ε

    -trifluoroacetyl-L-lysine in the presence of phosphorous pentoxide in N-methyl-2-pyrrolidone, to a temperature of between 150° and

    175°

    C. for between 0.25 and 5 hours, the concentration of phosphorous pentoxide is from 20% to 35% that of the lysine; and

    quenching the mixture with water.

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