摘要
应用连续流动微反应器技术,以2-(2-溴-4,5-二甲氧基苯基)-1,3-二噁烷和6-苄氧基-3,4-亚甲二氧基苯甲醛反应合成爵床脂素G关键中间体[2-(1,3-二噁烷-2-基)-4,5-二甲氧基苯基]-(2-苄氧基-4,5-亚甲二氧基苯基)甲醇,收率91.7%。与常规反应相比,温度由-78℃提升到0℃;反应时间由4 h缩短到20 min。反应条件温和,操作简便,安全高效。
Using the continuous flow microreactor technology, [2-(1,3-dioxolan-2-yl)-4,5-dimethoxyphenyl]- (2-benzyloxy-4,5-methylenedioxyphenyl) methol, the key intermediate ofjusticidin G, was synthesized from 2- (2-bromo- 4,5-dimethoxyphenyl)-1,3-dioxolane and 3,4-(methylenedioxy)benzaldehyde with a yield of 91.7 %. Compared with the conventional reaction, the reaction temperature rised from -78 C to 0 C, the reaction time reduced from 4 h to 20 min, and the reaction conditions were mild, safe and effective.
出处
《中国医药工业杂志》
CAS
CSCD
北大核心
2013年第4期341-343,共3页
Chinese Journal of Pharmaceuticals
基金
国家“重大新药创制”科技重大专项创新药物研究开发技术平台建设(2012ZX09301002-001)
原料药技术改造(2011ZX09203-001-16)项目
关键词
微反应器
爵床脂素G
中间体
合成
microreactor
justicidin G
intermediate
synthesis