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

Abstract: the disclosed embodiments detail improved methods for the synthesis of diketopiperazines from amino acids. in particular improved methods for the cyclocondensation and purification of n-protected 3,6-(aminoalkyl)-2,5-diketopiperazines from n-protected amino acids. disclosed embodiments describe methods for the synthesis of 3,6-bis-[n-protected aminoalkyl]-2,5-diketopiperazine comprising heating a mixture of an amino acid in the presence of a catalyst in an organic solvent. the catalyst is selected from the group comprising sulfuric acid, phosphoric acid, p-toluenesulfonic acid, 1-propylphosphonic acid cyclic anhydride, tributyl phosphate, phenyl phosphonic acid and phosphorous pentoxide among others. the solvent is selected from the group comprising: dimethylacetamide, n-methyl-2-pyrrolidone, diglyme, ethyl glyme, proglyme, ethyldiglyme, m-cresol, p-cresol, o-cresol, xylenes, ethylene glycol and phenol among others.

Inventor(s): JOHN J. FREEMAN, ADRIENNE STAMPER, MELISSA HEITMANN

CPC Classification: C07D241/08 (HETEROCYCLIC COMPOUNDS (macromolecular compounds ))

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