酪氨酸蛋白磷酸酶SHP-2抑制剂PHPS1及其类似物的合成  

Synthesis of Tyrosine Protein Phosphatases SHP-2 Inhibitor PHPS1 and Its Analogues

作　　者：崔志文[1] 蒋丝绒 闵真立[1] 杨凯文[1] 朱月[1] 胡霞敏[1] CUI Zhi-wen JIANG Si-rong MlN Zhen-li YANG Kai-wen ZHU Yue HU Xia-min(Department of Pharmacology, Wuhan University of Science and Technology, Wuhan 430065, Chin)

机构地区：[1]武汉科技大学医学院,湖北武汉430065

出　　处：《化学试剂》2017年第3期326-328,共3页Chemical Reagents

基　　金：武汉科技大学国家级大学生创新创业项目(201510488010)

摘　　要：以冰醋酸为溶剂,苯肼及其衍生物与取代酰基乙酸乙酯反应得到吡唑啉酮类中间体。然后再与由苯胺衍生物制备的重氮盐反应,最后得到苯基腙吡唑酮衍生物PHPS1及其类似物,并通过~1HNMR、IR和MS对其结构进行确证。为苯基腙吡唑酮类SHP-2抑制剂的合成提供了新思路。Phenylhydrazine and its derivatives reacted with ethyl substituted acylacetates to obtaina serial of pyrazolone intermediates in acetic acid which followed by reactions with the diazonium salts prepared from aniline derivatives,and the phenylhydrazonopyrazolone derivative PHPS1 and its analogues were synthesized.The structures of the products were confirmed by -1HNMR,IR and MS.This work gives a new idea on the synthesis of phenylhydrazonopyrazolone SHP-2 inhibitor.

关 键 词：SHP-2抑制剂 PHPS1 合成 

分 类 号：O621.3[理学—有机化学]