磷酸芦可替尼合成路线图解

Graphical synthetic routes to ruxolitinib phosphate

磷酸芦可替尼(ruxolitinib phosphate,1),中文化学名称为(R)-3-[4-(7H-吡咯[2,3-d]嘧啶-4-基)-1H-吡唑-1-基]3-环戊基丙腈磷酸盐,是蛋白酪氨酸激酶JAK1/JAK2的靶点抑制剂,可选择性抑制JAK2细胞增殖,降低磷酸化JAK2和STAT5的信号转导,抑制JAK-STAT通路活化,从而靶向性压低该通道异常增强的信号,具有良好的临床疗效[1-3]。

Ruxolitinib phosphate,as a protein tyrosine kinase JAK1/JAK2i nhibitor,was first developed and marketed by Incyte corpora-t ion and Novartis corporation in2011.A series of syntheticr outes of ruxolitinib phosphate were summarized,and their ad-v antages and disadvantages were analyzed in this paper.