基本信息:
- 专利标题： NOVEL PROCESS FOR SYNTHESIS OF A PHENOXY DIAMINOPYRIMIDINE COMPOUND
- 申请号：PCT/US2019/028014 申请日：2019-04-18
- 公开(公告)号：WO2019209607A1 公开(公告)日：2019-10-31
- 发明人： MALONEY, Kevin, M. , BASU, Kallol , CHUNG, John, Y.L. , DESMOND, Richard , DI MASO, Michael James , HUMPHREY, Guy, R. , LEE, Alfred, Y. , LEHNHERR, Dan , PENG, Feng , REN, Hong , WEISEL, Mark , ZHANG, Siwei , LARPENT, Patrick
- 申请人： MERCK SHARP & DOHME CORP. , MSD WERTHENSTEIN BIOPHARMA GMBH , MALONEY, Kevin, M. , BASU, Kallol , CHUNG, John, Y.L. , DESMOND, Richard , DI MASO, Michael James , HUMPHREY, Guy, R. , LEE, Alfred, Y. , LEHNHERR, Dan , PENG, Feng , REN, Hong , WEISEL, Mark , ZHANG, Siwei , LARPENT, Patrick
- 申请人地址： 126 East Lincoln Avenue Rahway, New Jersey 07065-0907 US
- 专利权人： MERCK SHARP & DOHME CORP.,MSD WERTHENSTEIN BIOPHARMA GMBH,MALONEY, Kevin, M.,BASU, Kallol,CHUNG, John, Y.L.,DESMOND, Richard,DI MASO, Michael James,HUMPHREY, Guy, R.,LEE, Alfred, Y.,LEHNHERR, Dan,PENG, Feng,REN, Hong,WEISEL, Mark,ZHANG, Siwei,LARPENT, Patrick
- 当前专利权人： MERCK SHARP & DOHME CORP.,MSD WERTHENSTEIN BIOPHARMA GMBH,MALONEY, Kevin, M.,BASU, Kallol,CHUNG, John, Y.L.,DESMOND, Richard,DI MASO, Michael James,HUMPHREY, Guy, R.,LEE, Alfred, Y.,LEHNHERR, Dan,PENG, Feng,REN, Hong,WEISEL, Mark,ZHANG, Siwei,LARPENT, Patrick
- 当前专利权人地址： 126 East Lincoln Avenue Rahway, New Jersey 07065-0907 US
- 代理机构： MERCK SHARP & DOHME CORP.
- 优先权： US62/661,362 20180423; US62/662,991 20180426
- 主分类号： A61K31/505
- IPC分类号： A61K31/505
摘要：
Disclosed herein is a novel process for preparing Compound A free base, 5-((2,4-diaminopyrimidin-5-yl)oxy)-4-isopropyl-2-methoxybenzenesulfonamide, and a citrate salt of Compound A with simplified chemistry and a high overall yield: Compound A. In one embodiment, the overall yield from the starting material 2-isopropylphenol to Compound A citrate salt is greater than 50%. In another embodiment, the overall yield is greater than 60%. Also disclosed herein are novel salts and solvates of Compound A.
IPC结构图谱:
| A | 人类生活必需 |
| --A61 | 医学或兽医学；卫生学 |
| ----A61K | 医用、牙科用或梳妆用的配制品 |
| ------A61K31/00 | 含有机有效成分的医药配制品 |
| --------A61K31/33 | .杂环化合物 |
| ----------A61K31/335 | ..仅有氧作为环杂原子的，例如制霉色基素 |
| ------------A61K31/40 | ...有仅以1个氮作为环杂原子的五元环的，例如舒必利、琥珀酰亚胺、托尔米丁、甲氧吡丁苯 |
| --------------A61K31/505 | ....嘧啶；氢化嘧啶，例如甲氧苄啶 |