摘要
BI-167107是一种新的长效β2肾上腺素受体(β2-AR)激动剂,在鉴定G蛋白偶联受体(GPCR)/配体络合物的结构方面具有重要应用.以2-硝基间苯二酚为原料,经过七步反应,合成了目标化合物,其结构经1H NMR,13C NMR和MS确证.此合成路线的优点是避免了使用有毒试剂,可以便捷地用于制备较大量的BI-167107及结构相近的苯并噁嗪类化合物.
BI-167107 is a new long-acting β2-adrenergic receptor （β2-AR） agonist, and has important application in deter- mining the critical structures of receptor/ligand proteins complex of G-protein-coupled receptor （GPCR）. By employing 2-nitroresorcinol as starting material, a practical synthetic route for BI-167107 has been developed, involving 7-step reactions. The structure of the target molecule has been confirmed by 1H NMR, 13C NMR and MS techniques. The advantages of the synthetic route include avoiding use of toxic reagents and being suitable for scale up preparation of BI-167107 and other ben- zoxazine derivatives.
出处
《有机化学》
SCIE
CAS
CSCD
北大核心
2013年第3期634-639,共6页
Chinese Journal of Organic Chemistry
基金
国家自然科学基金(Nos.21272029
81272982)资助项目~~
