17628-76-1Relevant articles and documents
Single-Step Modular Synthesis of Unsaturated Morpholine N-Oxides and Their Cycloaddition Reactions
Son, Jongwoo,Kim, Ki Hwan,Mo, Dong-Liang,Wink, Donald J.,Anderson, Laura L.
supporting information, p. 3059 - 3063 (2017/03/14)
A single-flask procedure for the generation of α-keto-N-alkenylnitrones through a Chan–Lam coupling and subsequent spontaneous 6π electrocyclization of these intermediates for the synthesis of 2H-1,4-oxazine N-oxides has been developed for a variety of α-ketooximes and alkenylboronic acids. This transformation provides a new approach to C-substituted unsaturated morpholine derivatives that are poised to undergo further functionalization for the preparation of a diverse array of novel heterocyclic structures. The scope of the new method for the synthesis of 2H-1,4-oxazine N-oxides is discussed, in addition to initial studies describing the cycloaddition reactivity of these new heterocyclic intermediates.
Copper-catalyzed direct amination of 1,2,3-triazole N-oxides by C-H activation and C-N coupling
Zhu, Jiayi,Kong, Yubo,Lin, Feng,Wang, Baoshuang,Chen, Zhengwang,Liu, Liangxian
supporting information, p. 1507 - 1515 (2015/03/04)
An efficient approach for the synthesis of 4-amino-2-aryl- 1,2,3-triazole derivatives has been developed through the copper-catalyzed direct C-H amination of 2-aryl-1,2,3-triazole N-oxides under mild reaction conditions. Various amines, including primary and secondary aliphatic and aromatic amines, can be employed as effective coupling partners. The general performance of our method was also demonstrated by the oxidative amination of thiazole and imidazole N-oxides.
Synthesis and biological activities of 2,4-diaminopteridine derivatives
Ma, Fei,Lue, Gang,Zhou, Wei-Fen,Wang, Qiu-Juan,Zhang, Yi-Hua,Yao, Qi-Zheng
experimental part, p. 274 - 280 (2009/09/06)
Substituted 2,4-diaminopteridine derivatives 10a-10l were prepared in moderate to good yield. Their structures were confirmed by 1H-NMR and MS spectroscopy, as well as by elemental analysis. Their inhibitory properties against inducible nitric oxide synthase (iNOS) were evaluated in vitro. Biological tests indicated that compound 10a, 10d, 10e, 10h, 10i, and 10l showed potent inhibitory activities similar to that of methotrexate (MTX), while the activities of compound 10b, 10c, 10f, 10g, 10j, and 10k are stronger than MTX. Two compounds, i. e., 10b (IC50 = 18.85 μM) and 10i (IC 50 = 24.08 μM) were further studied for their effect on septic shock in rats and immunologically liver injured mice (in vivo). The results demonstrated that 10b and 10i had the capacity to increase the blood pressure in septic shock and showed notable protective activities on immunological hepatic injury.