1425045-01-7
1425045-01-7 結(jié)構(gòu)式
基本信息
1,5-二甲基-6-氧代-1,6-二氫吡啶-3-硼酸頻哪醇酯
1,3-二甲基-5-(4,4,5,5-四甲基-1,3,2-二氧雜硼烷-2-基)吡啶-2(1H)-酮
1,3-二甲基-5-(4,4,5,5-四甲基-1,3,2-二氧雜硼雜環(huán)戊烷-2-基)-2(1H)-吡啶酮
1,3-DIMETHYL-5-(4,4,5,5-TETRAMETHYL-1,3,2-DI氧BENZALDEHYDE-2-YL)-1,2-DIHYDROPYRIDINE-2-ONE
1,3-Dimethyl-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-2(1H)-pyridinone
1,3-diMethyl-5-(4,4,5,5-tetraMethyl-1,3,2-dioxaborolan-2-yl)pyridin-2(1H)-one
1,3-dimethyl-5-(tetramethyl-1,3,2-dioxaborolan-2-yl)-1,2-dihydropyridin-2-one
1,3-Dimethyl-5-(4,4,5,5-tetramethyl-[1,3,2]dioxaborolan-2-yl)-1H-pyridin-2-one
2(1H)-Pyridinone, 1,3-dimethyl-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-
制備方法
51417-13-1
73183-34-3
1425045-01-7
以5-溴-1,3-二甲基吡啶-2(1H)-酮和聯(lián)硼酸頻那醇酯為原料合成1,3-二甲基吡啶-2(1H)-酮-5-頻哪醇硼酸酯的一般步驟如下:首先,將氮?dú)馔ㄈ攵和橹羞M(jìn)行脫氣處理。隨后,將脫氣后的二惡烷溶液(2.0 mL)加入到含有5-溴-1,3-二甲基吡啶-2(1H)-酮(75 mg,0.37 mmol)、雙(頻哪醇)二硼(113 mg,0.445 mmol)和KOAc(109 mg,1.11 mmol)的混合物中。接著,加入催化劑PdCl2(dppf)·CH2Cl2(30 mg,0.037 mmol)。將反應(yīng)混合物在85℃下加熱反應(yīng)16小時(shí)。反應(yīng)完成后,用EtOAc稀釋反應(yīng)混合物,并通過(guò)Celite墊過(guò)濾。最后,將濾液在真空下濃縮,得到粗產(chǎn)物1,3-二甲基吡啶-2(1H)-酮-5-頻哪醇硼酸酯(169 mg,0.678 mmol,定量收率),為棕色油狀物。
參考文獻(xiàn):
[1] Patent: WO2016/196644, 2016, A1. Location in patent: Paragraph 709; 710
[2] Journal of Medicinal Chemistry, 2016, vol. 59, # 10, p. 4462 - 4475
[3] Patent: WO2014/78323, 2014, A1. Location in patent: Paragraph 00584
[4] Patent: US2018/44335, 2018, A1. Location in patent: Paragraph 0459-0460
[5] Patent: WO2018/102452, 2018, A2. Location in patent: Paragraph 693; 694
