一种替代方法通过改进的铜催化循环合成西尔德纳菲尔
Abdullajon Odilov1,2, Xudong Gong3, Hongjian Qin2,4
1State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China.
The Journal of organic chemistry
|May 6, 2024
概括
通过铜催化合反应,创造了新型的,高效的西尔德纳菲尔及其衍生物合成. 这种方法避免了苛刻的化学物质和昂贵的催化剂,为这些重要的化合物提供了更绿色,更具成本效益的生产途径.
科学领域:
- 有机化学 有机化学
- 药用化学 医学化学
- 合成化学 合成化学
背景情况:
- 西尔德纳菲尔是一种广泛使用的药物剂.
- 现有的锡德纳菲尔合成途径通常涉及多个步骤,苛刻的试剂和昂贵的催化剂.
- 需要更高效和可持续的合成方法.
研究的目的:
- 开发一种易于和高效的合成途径,用于西尔德纳菲尔及其衍生物.
- 建立一种无合体的乌尔曼型铜催化合反应,用于构建pyrrazolo[4,3-d]pyrimidin-7-one核心结构.
主要方法:
- 采用了一种单,无带的乌尔曼型铜催化合反应.
- 使用了关键的构建块,-pyrazole部分16c,2-ethoxybenzamidine,和2-ethoxy-5-[(4-methylpiperazin-1-yl) sulfonyl]benzamidine. 这些都是使用的.
- 反应被优化为融合合成.
主要成果:
- 席尔德纳菲尔及其衍生物的合成产量分别为79%和82%的高产量.
- 开发的方法规避了化时需要酸/硫酸的需求.
- 该过程避免了用于减少和合剂的昂贵的催化剂.
结论:
- 已经成功开发了一种新的,高效的和融合的合成途径,用于西尔德纳菲尔及其衍生物.
- 这种方法在现有过程中提供了显著的优势,因为它消除了危险的试剂和昂贵的催化剂.
- 简单的合成途径为制药生产提供了更绿色,更具成本效益的方法.
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