α-酰氨基烃基膦酸二乙酯的合成及其分子结构的测定

Synthesis of Diethyl N-Acyl-α-aminoalkylphosphonates and Determination of their Molecular Structures

氨基膦酸是继氨基酸、氨基磺酸后在生物体中发现的第三类氨基酸,它在生物体中的分布、代谢和功能正在进一步研究中。目前人们正积极开展合成各种天然氨基酸的磷类似物——α-氨基烃基膦酸的肽,且巴发现这类合成肽具有重要的生理活性。在膦肽合成中。

A facile one-pot procedure for the preparation of diethyl N-carbobenzyoxy-or N-acetyl-α-aminoalbylphosphonates from the condensation of relevant aldehydes,amides andphosphorus trichloride was described.A tentative reaction mechanism was proposed anddiscussed.The crystal and molecular structure of dietheyl N-acetyl-α-amino-γ-methyl bu- tylphosphonate(g)and by product N-[α-isopropyl-5-methylhexadienyl-(1,3)]-acetamide(h)were determined by X-ray diffraction.The crystal of(g)belongs to a P(?) space groupwith lattice parameters:α=8.688(4),b=8.990(3),c=10.309(2);α=87.89(2),β=83.63(2),γ=88.27(3)and the crystal of(h)belongs to Pna 2_1 space group,the latlice parame-ters are α= 9.326(4),b=14.276(3),c=9.843(2).