Abstract

Phosphinic isosteres of leucylglycine and isoleucylglycine were obtained by amidoalkylation of (3-benzyloxy-3-oxopropyl)phosphonous acid bearing the structural isostere fragment of glycine benzyl ester in acetyl chloride. A three-component amide version of the Kabachnik–Fields reaction involving methyl (benzyl) carbamates and 2(3)-methylbutanals was studied. The reaction proceeded under the conditions of acylation of the starting (3-benzyloxy-3-oxopropyl)phosphonous acid and in situ generation of a bisacetyl derivative of the three-coordinated phosphorus, the formation of which was detected using NMR ³¹Р.

中文翻译：

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亮氨酰和异亮氨酰甘氨酸的膦等聚体的合成

摘要

通过在乙酰氯中将具有甘氨酸苄基酯的结构等排异构体片段的（3-苄氧基-3-氧代丙基）亚膦酸进行氨基烷基化，获得亮氨酰甘氨酸和异亮氨酰甘氨酸的膦酰基等排体。研究了涉及氨基甲酸苄酯和2（3）-甲基丁醛的Kabachnik-Fields反应的三组分酰胺形式。起始（3-苄氧基-3-氧代丙基）的酰化亚膦酸的条件下和进行该反应原位生成三协调磷bisacetyl衍生物，用NMR检测，其形成³¹ Р.