申请人:——
公开号:US20020173664A1
公开(公告)日:2002-11-21
This invention provides amino acid N-carboxyanhydrides, each of which has an N-acyl substituent on its nitrogen atom, is represented by the following formula (1):
1
readily reacts with nucleophilic reagents such as free amino acids, alcohols, anions or the like, and are intermediates useful for the high-yield production of amino acid derivatives, optically active compounds, peptides, polypeptides and the like useful in many fields lead by the fields of pharmaceuticals and agrochemicals, and also provides a process for the production of the amino acid N-carboxyanhydrides. Further, the present invention also provides a process for the production of diamides, which uses the compounds of the formula (1) and amine derivatives represented by the following formula (7):
2
These diamides can also be suitably used for the production of amino acid derivatives, optically active compounds, peptides, polypeptides and the like.
本发明提供了氨基酸N-羧酸酐,每个酐都在其氮原子上具有N-酰基取代基,由以下公式(1)表示:1可以与自由氨基酸、醇、阴离子等亲核试剂轻松反应,是用于高产率生产氨基酸衍生物、光学活性化合物、肽、多肽等在制药和农化领域等多个领域有用的中间体,并提供了一种制备氨基酸N-羧酸酐的方法。此外,本发明还提供了一种使用公式(1)所述化合物和以下公式(7)所表示的胺衍生物的二酰胺的制备方法:2这些二酰胺也可适用于生产氨基酸衍生物、光学活性化合物、肽、多肽等。