5028-17-1

基本信息
2-(4-甲基哌嗪)-3-氨基吡啶
2-(4-甲基哌嗪-1-基)吡啶-3-胺
2-(4-METHYLPIPERAZINO)-3-PYRIDINAMINE
1-(3-amino-2-pyridyl)-4-methyl-piperazin
1-(3-amino-2-pyridyl)-4-methylpiperazine
2-(4-METHYL-1-PIPERAZINYL)-3-PYRIDINAMINE
3-Pyridinamine, 2-(4-methyl-1-piperazinyl)-
2-(4-methyl-piperazin-1-yl)-pyridin-3-ylamine
物理化學(xué)性質(zhì)
制備方法

5028-15-9

5028-17-1
以1-甲基-4-(3-硝基-2-吡啶基)哌嗪為原料合成2-(4-甲基哌嗪)-3-氨基吡啶的一般步驟:準(zhǔn)備2-(4-甲基哌嗪-1-基)-3-硝基吡啶(PP26,0.50g,2.25mmol)、甲酸銨(1.00g,15.85mmol)和10% Pd/C(0.050g)的甲醇(20mL)溶液。在室溫下攪拌反應(yīng)混合物1小時,隨后通過硅藻土(Celite?)過濾并濃縮濾液。將殘余物溶解于乙酸乙酯中,依次用碳酸鉀水溶液和鹽水洗滌,無水硫酸鎂干燥后濃縮,得到0.35g(產(chǎn)率81%)的2-(4-甲基哌嗪)-3-氨基吡啶(PP24),為紫色油狀物,未經(jīng)進(jìn)一步純化直接用于下一步反應(yīng)。產(chǎn)物經(jīng)核磁共振氫譜(CDCl3)確認(rèn):δ 7.77(dd,J = 4.6, 1.7Hz,1H),6.90(dd,J = 7.5, 1.7Hz,1H),6.79(dd,J = 7.9, 5.0Hz,1H),3.71(br s,2H),3.15(br s,4H),2.57(br s,4H),2.34(s,3H)。
參考文獻(xiàn):
[1] Patent: WO2006/48727, 2006, A1. Location in patent: Page/Page column 72-73
[2] Patent: WO2013/40215, 2013, A1. Location in patent: Paragraph 00304
[3] Patent: WO2018/75858, 2018, A1. Location in patent: Paragraph 0335; 0337