Synthesis of Tofacitinib Citrate
Author(s): ZHAO Fanglu, CHEN Guohua, YAO Shilun, ZHANG Zhenxia
Pages: 201-204,253
Year: 2014 Issue: 3
Journal: Chinese Journal of Pharmaceuticals
Keyword: tofacitinib citrate; anti-rheumatoid arthritis drug; synthesis;
Abstract: 3-氨基-4-甲基吡啶与碳酸二甲酯反应,再经氢化、与溴苄反应、LiAlH4还原及成盐得顺-(1-苄基-4-甲基哌啶-3-基)甲胺二盐酸盐,经L-DTTA拆分后与4-碘-7H-吡咯并[2,3-d]嘧啶经亲核取代反应、脱苄基、缩合后成枸橼酸盐得枸橼酸托法替尼,总收率约9％(以3-氨基-4-甲基吡啶计).
Pages: 201-204,253
Year: 2014 Issue: 3
Journal: Chinese Journal of Pharmaceuticals
Keyword: tofacitinib citrate; anti-rheumatoid arthritis drug; synthesis;
Abstract: 3-氨基-4-甲基吡啶与碳酸二甲酯反应,再经氢化、与溴苄反应、LiAlH4还原及成盐得顺-(1-苄基-4-甲基哌啶-3-基)甲胺二盐酸盐,经L-DTTA拆分后与4-碘-7H-吡咯并[2,3-d]嘧啶经亲核取代反应、脱苄基、缩合后成枸橼酸盐得枸橼酸托法替尼,总收率约9％(以3-氨基-4-甲基吡啶计).
Related Articles