Department of Chemistry, Temple University , Philadelphia, Pennsylvania 19122, United States.
J Org Chem. 2017 Mar 17;82(6):3223-3231. doi: 10.1021/acs.joc.6b01773. Epub 2017 Feb 27.
Derivatives of 4-hydantoin-proline have been synthesized via a direct two-step alkylation method. This method is valuable in the development of applications of N,N'-disubstituted hydantoin bearing α-amino acids by improving yields, reducing the time and number of steps required to synthesize these substituted molecules, and enabling late stage functionalization of spiroligomer termini. Over 20 unique electrophiles have been tested, highlighting the inherent versatility of this chemistry.
通过直接的两步烷基化方法合成了 4-海因基脯氨酸衍生物。这种方法在开发含有α-氨基酸的 N,N'-二取代海因的应用方面具有价值,通过提高产率、减少合成这些取代分子所需的时间和步骤数,以及实现螺环寡聚物末端的后期功能化,使该方法具有内在的多功能性。已经测试了超过 20 种独特的亲电试剂。