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-N- Amino acid carboxy anhydride having a substituent at the nitrogen atom

机译:-N-在氮原子上具有取代基的氨基酸羧酸酐

摘要

PROBLEM TO BE SOLVED: To provide a new amino acid-N-carboxyanhydride with an N-acyl substituent on the nitrogen atom as an important intermediate considered as highly useful in various fields including medicinal and agrochemical fields and having been unavailable by conventional production techniques, to provide a method for producing the amino acid-N-carboxyanhydride, and to provide a method for producing an inexpensive diamide compound in few steps by the use of the above new compound without causing problems such as racemization. SOLUTION: This new amino acid-N-carboxyanhydride of formula (1) is highly reactive with a nucleophilic reagent such as a free amino acid, an alcohol or anion and serves as an intermediate useful for producing in high yield amino acid derivatives, optically active compounds, peptides, polypeptides, etc., each useful in various fields including medicinal and agrochemical fields. The 2nd objective method for producing the above new compound, and the other objective method for producing a diamide involving using the new compound of formula (1) and an amine derivative of formula (7), are also provided, respectively.
机译:解决的问题:提供一种新的氨基酸-N-羧基酸酐,其在氮原子上具有N-酰基取代基,作为重要的中间体,被认为在医药和农业化学等各个领域都非常有用,并且是常规生产技术所不具备的,提供一种制备氨基酸-N-羧基酸酐的方法,并提供一种通过使用上述新化合物以很少的步骤制备廉价的二酰胺化合物的方法,而不会引起外消旋等问题。解决方案:这种新型的式(1)氨基酸-N-羧基酸酐与亲核试剂(例如游离氨基酸,醇或阴离子)具有高度反应性,并用作中间体,可用于高产率地生产具有光学活性的氨基酸衍生物化合物,肽,多肽等,各自可用于包括医学和农业化学领域在内的各个领域。还分别提供了制备上述新化合物的第二目的方法和涉及使用式(1)的新化合物和式(7)的胺衍生物的制备二酰胺的另一目的方法。

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