| 摘要 |
<p>A process is described for the preparation of alkylated azaglycine derivatives of the formula I, X-(A)n-N(R)-NH-CO-NH2, (I> in which X represents an amino protective group, C1-C8-alkanoyl, C8-C14-arylcarbonyl or C6-C14-aryl-C1-C4-alkanoyl; A represents amino acid radicals or imino acid radicals which are optionally protected at the third function; n represents 0 - 10, where X is C1-C8-alkanoyl, C6-C14-arylcarbonyl or C6-C14-aryl-C1-C14-alkanoyl if n = 0, and R represents C1-C8-alkyl, C6-C14-aryl-C1-C4-alkanoyl or C5-C12-heteroaryl-C1-C4-alkanoyl, characterised in that a compound of the formula X-(A)n-NH-NH-CO-NH2, in which X, A and n have the abovementioned meanings, are reacted with a primary or secondary alcohol and excess DEAD and a tri-C1-C6-alkylphosphine, tri-C6-C14-arylphosphine or pyridyl-di-C6-C14-arylphosphine, it being possible for the aryl moiety to be optionally substituted by di-C1-C4-alkylamino, in an ether at 0 DEG C to 30 DEG C, and the amino protective group X is optionally eliminated, with the proviso that X is not Fmoc if tri-n-butylphosphine is used.</p> |
