(2 S,5 S)-2-(2-(二苯基膦基)苯基)-3,5-二取代基咪唑啉-4-酮的合成

Synthesis of(2 S,5 S)-2-(2-(Diphenylphosphonyl)Phenyl)-3,5-Disubstituted Imidazoline-4-ones

随着金属催化不对称合成研究的兴起,研究人员对手性配体的需求日趋迫切,以简便的方式获得高效的手性配体一直是金属催化不对称反应研究的重点之一,其中包括含氮,磷等含杂原子的膦配体。这些配体广泛地用于C—C、C—N及C—O的构建和不对称氢化反应中,展现出了可观的研究及应用价值。以α-氨基酸为起始原料,在三光气作用下得到酸酐类中间体,随后经酰胺化、缩合两步反应,成功以26.4%~33.8%收率得到(2 S,5 S)-2-(2-(二苯基膦基)苯基)-3,5-二取代基咪唑啉-4-酮类化合物。

With the rising interests on metal-catalyzed asymmetric synthesis,researchers found the demand for chiral ligands is increasingly urgent.One of the key points of research on metal catalyzed asymmetric reactions is to obtain efficient chiral ligands such as phosphine ligands which containing nitrogen,phosphorus or other heteroatoms.Those ligands were widely used in construction of C—C bond,C—N bond,C—O bond and metal catalyzed asymmetric hydrogenation reactions,which proves their importance in both academy research and application.The(2 S,5 S)-2-(2-(diphenylphosphonyl)dhenyl)-3,5-disubstituted imidazoline-4-ones were obtained fromα-amino acid as starting material under the action of triphosgene,followed by two steps of amidation and condensation in 26.4%~33.8%yield.