公开(公告)号：US20210363098A1

公开(公告)日：2021-11-25

申请号：US17325291

申请日：2021-05-20

申请人： University of Georgia Research Foundation, Inc.

发明人： David Crich ,  Asiri Hettikankanamalage ,  Jarvis Hill

IPC分类号： C07C239/20 ,  C07B43/04 ,  C07D211/94 ,  C07D215/58 ,  C07D265/30 ,  C07D217/08 ,  C07D209/08 ,  C07D471/08 ,  C07H1/00 ,  C07C247/04 ,  C07D241/04 ,  C07D213/74 ,  C07D207/46 ,  C07H17/02 ,  C07H17/00 ,  C07D275/04

摘要： In one aspect, the disclosure relates to a method for the direct synthesis of complex N,N,O-trisubstituted hydroxylamines by N—O bond formation. In another aspect, the method can successfully be employed using a wide variety of commercially available alcohols and secondary amines and enables the construction of large fragment-based libraries of trisubstituted hydroxylamines for drug discovery purposes. Also disclosed are N,N,O-trisubstituted hydroxylamines having low basicity, high stability at ambient temperatures, and an inherent lack of reactivity towards acetylating and sulfonylating enzymes that confer mutagenicity on less-substituted hydroxylamines.

公开(公告)号：US11912647B2

公开(公告)日：2024-02-27

申请号：US17325291

申请日：2021-05-20

申请人： University of Georgia Research Foundation, Inc.

发明人： David Crich ,  Asiri Hettikankanamalage ,  Jarvis Hill

IPC分类号： C07C239/20 ,  C07D207/46 ,  C07B43/00

CPC分类号： C07C239/20 ,  C07B43/00 ,  C07D207/46

摘要： In one aspect, the disclosure relates to a method for the direct synthesis of complex N,N,O-trisubstituted hydroxylamines by N—O bond formation. In another aspect, the method can successfully be employed using a wide variety of commercially available alcohols and secondary amines and enables the construction of large fragment-based libraries of trisubstituted hydroxylamines for drug discovery purposes. Also disclosed are N,N,O-trisubstituted hydroxylamines having low basicity, high stability at ambient temperatures, and an inherent lack of reactivity towards acetylating and sulfonylating enzymes that confer mutagenicity on less-substituted hydroxylamines.