目的 設(shè)計合成吡咯并嘧啶類化合物并研究其抑制JAK3激酶的活性。方法 以4-氯-7H-吡咯并[2,3-d]嘧啶為原料，經(jīng)過取代、氨基脫保護(hù)和N-酰化反應(yīng)合成兩類（Ⅰ_a和Ⅰ_b）吡咯并嘧啶類化合物，經(jīng)體外細(xì)胞試驗(yàn)測定其對JAK3激酶的抑制活性。結(jié)果 設(shè)計并合成了8個新化合物，結(jié)構(gòu)經(jīng)¹H-NMR和HR-MS確證。初步活性測試結(jié)果顯示Ⅰ_a-1和Ⅰ_b-3對JAK3的抑制強(qiáng)度與陽性對照藥tofacitinib相近。結(jié)論 目標(biāo)化合物對JAK3依賴的DAUDI細(xì)胞抑制活性較好，對非JAK3依賴的BT-20細(xì)胞抑制作用弱。

Objective To design and synthesize pyrrolopyrimidines and study their JAK3 inhibitory activities. Methods The two kinds of pyrrolopyrimidines (I_a and I_b)were synthesized from 4-chloro-7H-pyrrolo[2,3-d]pyrimidine via substitution reaction, amino deprotection, and N-acetylation reaction. Their JAK3 inhibitory activities were tested by in vitro cell assay. Results Eight novel compounds were synthesized and their structures were confirmed by ¹H-NMR and HR-MS. The in vitro activity experiments showed that compounds I_a-1 and I_b-3 had good inhibition against JAK3, and it was near to control drug tofacitinib. Conclusion Target compounds had good inhibition on JAK3-depended DAUDI cells, and rarely inhibition on non-JAK3-depended BT-20 cells.