[3+2+1]反应合成1,3-噁嗪衍生物

[3+2+1]reaction synthesis of 1,3-oxazines

噁嗪衍生物按照氮原子和氧原子的位置不同,可分为1,2-噁嗪、1,3-噁嗪、1,4-噁嗪三种不同的骨架,是一类重要的医药母体结构.1,3-噁嗪具有抗癌、抗炎、抗抑郁等活性,在三种噁嗪骨架中关注度最高.选用1-芳基-5-氨基吡唑和芳酮醛水合物为原料,在醋酸条件下,通过[3+2+1]反应,合成了6例1,3-噁嗪衍生物,并对合成产物作相应的表征,拓展了室温条件下该衍生物的合成.

According to the different positions of nitrogen and oxygen atoms,oxazines can be divided into three different skeletons of 1,2-oxazine,1,3-oxazine,and 1,4-oxazine,which is an important medical matrix structure.1,3-oxazines have the activities of anti-cancer,anti-inflammatory and anti-depressant,which have the highest attention among the three oxazine skeletons.Using 1-aryl-5-aminopyrazole and arylketal hydrate as raw materials,6 cases of 1,3-oxazines were synthesized by[3+2+1]reaction under acetic acid conditions,and the synthetic products were characterized accordingly,which extended the synthesis of this derivative at room temperature.