用于合成含咪唑并[1,2-a]吡啶结构的化合物,可能作为药物中间体或农药活性成分
医药; 农药
路线1:微波辅助合成
- 步骤: 将2-氨基吡啶(1mmol)和α-溴酮(2)(1mmol)的混合物置于微波合成仪小瓶中,在65℃、120W和1巴压力下微波辐射15-20分钟,冷却至室温后,经氧化铝(溶剂:二氯甲烷)柱色谱纯化得到产物
- 条件: 65℃; 120W; 1巴压力; 微波辐射; 15-20分钟
- 收率: 85%
- 参考文献: [1] Journal of Chemical Research, 2016, vol. 40, #9, p.529-531; [2] Synthetic Communications, 2005, vol.35, #7, p.901-906; [3] Tetrahedron Letters, 2017, vol.58, #28, p.2771-2773; [4] Bulletin of the Chemical Society of Japan, 1999, vol.72, #6, p.1327-1334; [5] European Journal of Organic Chemistry, 2014, vol.2014, #21, p.4643-4650; [6] Australian Journal of Chemistry, 1995, vol.48, #5, p.1031-1038; [7] European Journal of Organic Chemistry, 2016, vol.2016, #20, p.3373-3379; [8] Synthetic Communications, 2016, vol.46, #21, p.1741-1746; [9] Organic Letters, 2017, vol.19, #9, p.2226-2229; [10] European Journal of Organic Chemistry, 2018, vol.2018, #26, p.3432-3436
路线2:碘催化合成
- 步骤: 将2-氨基吡啶(0.25mmol)、取代的苯乙酮(0.25mmol)、碘(20mol%,13mg)和环己烷(2mL)置于25mL圆底烧瓶中,60℃搅拌15分钟,反应后用30mL水稀释,乙酸乙酯萃取有机层,Na₂SO₄干燥后减压浓缩,经石油醚和乙酸乙酯柱色谱纯化
- 条件: 60℃; 环己烷溶剂; 15分钟; 碘催化(20mol%)
- 收率: 65%
- 参考文献: [1] Molecules, 2012, vol.17, #11, p.13368-13375; [2] Journal of the Chinese Chemical Society, 2004, vol.51, #6, p.1377-1380; [3] Synthetic Communications, 2018, vol.48, #9, p.1076-1084; [4] Advanced Synthesis and Catalysis, 2013, vol.355, #9, p.1741-1747; [5] Advanced Synthesis and Catalysis, 2013, vol.355, #11-12, p.2217-2221; [6] European Journal of Organic Chemistry, 2015, vol.2015, #29, p.6526-6533; [7] Journal of Organic Chemistry, 2018, vol.83, #14, p.7331-7340