89937-26-8

基本信息
1-(6-氯-3-噠嗪基)-4-羥基哌啶
1-(6-CHLORO-3-PYRIDAZINYL)-4-PIPERIDINOL
1-(6-Chloro-3-pyridazinyl)piperidin-4-ol
4-Piperidinol, 1-(6-chloro-3-pyridazinyl)-
1-(6-Chloropyridazin-3-yl)piperidin-4-ol95%
1-(6-Chloropyridazin-3-yl)-4-hydroxypiperidine
1-(6-Chloro-pyridazino-3-yl)-4-hydroxypiperidine
1-(6-Chloro-3-pyridazinyl)-4-piperidinol ISO 9001:2015 REACH
物理化學(xué)性質(zhì)
制備方法

5382-16-1

141-30-0

89937-26-8
一般步驟:在密封容器中,將3,6-二氯噠嗪(1當(dāng)量)、4-羥基哌啶(1當(dāng)量)及非質(zhì)子堿(如Et3N或K2CO3,2-3當(dāng)量)溶于DMSO或EtOH中,加熱反應(yīng)直至通過TLC或HPLC監(jiān)測(cè)顯示原料完全消耗。反應(yīng)完成后,進(jìn)行后處理:部分蒸發(fā)反應(yīng)混合物,隨后加入水,過濾收集析出的固體產(chǎn)物(適用于如37的情況);或者將部分蒸發(fā)的反應(yīng)混合物在EtOAc與水之間分配,水層用EtOAc萃取數(shù)次以確保完全提取。合并有機(jī)層,經(jīng)無水Na2SO4干燥后,減壓濃縮得到粗產(chǎn)物,最后通過柱色譜法進(jìn)行純化。
參考文獻(xiàn):
[1] Bioorganic and Medicinal Chemistry, 2016, vol. 24, # 8, p. 1819 - 1839
[2] Patent: WO2016/54388, 2016, A1. Location in patent: Page/Page column 57
[3] Journal of Medicinal Chemistry, 1984, vol. 27, # 8, p. 1077 - 1083
[4] Bioorganic and Medicinal Chemistry Letters, 2011, vol. 21, # 24, p. 7281 - 7286
[5] Patent: WO2008/46226, 2008, A1. Location in patent: Page/Page column 42