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    • 4. 发明申请
    • PREPARATION OF (S)-N-(5-((R)-2-(2,5-DIFLUOROPHENYL)PYRROLIDIN-1-YL)PYRAZOLO[1,5-A]PYRIMIDIN-3-Y L)-3-HYDROXYPYRROLIDINE-1-CARBOXAMIDE
    • (S)-N-(5 - ((R)-2-(2,5-二氟苯基)吡咯烷-1-基)吡唑并[1,5-a]嘧啶-3-基)-3-羟基吡咯烷 - -1-甲酰胺
    • WO2017201241A1
    • 2017-11-23
    • PCT/US2017/033257
    • 2017-05-18
    • REYNOLDS, MarkEARY, Charles ToddSPENCER, StaceyJUENGST, DerrickHACHE, BrunoJIANG, YutongHAAS, JuliaANDREWS, Steven W.
    • REYNOLDS, MarkEARY, Charles ToddSPENCER, StaceyJUENGST, DerrickHACHE, BrunoJIANG, YutongHAAS, JuliaANDREWS, Steven W.
    • C07D487/04A61K31/5025A61P35/00
    • Process for preparing (S)-N-(5-((R)-2-(2,5-difluorophenyl)pyrrolidin-l- yl)pyrazolo[l,5-a] pyrimidin-3-yl)-3-hydroxypyrrolidine-l-carboxamide (formula I) or a salt thereof by reacting phenyl(5-((R)-2-(2,5- difluorophenyl)pyrrolidin-l-yl)-3,3a-dihydropyrazolo[l,5-a]pyrimidin-3- yl)carbamate or a similar derivative (formula 13) with (S)-pyrrolidin-3- ol (formula 14). Process for preparing phenyl(5-((R)-2-(2,5-difluorophenyl)pyrrolidin-l- yl)-3,3a-dihydropyrazolo[l,5-a]pyrimidin-3-yl)carbamate (formula 13) or a similar derivative by reduction of (R)-5-(2-(2,5-difluorophenyl) pyrrolidin-l-yl)-3-nitropyrazolo[l,5-a]pyrimidine (formula 11) to (R) -5-(2-(2,5-difluorophenyl)pyrrolidin-l-yl)pyrazolo[l,5-a]pyrimidin-3- amine (formula 12). Process for preparing (R)-2-(2,5-difluorophenyl)pyrrolidine(R) -2-hydroxysuccinate (formula 10) by treating (R)-N-((R)-l-(2,5- difluorophenyl)-3-(l,3-dioxan-2-yl)propyl)-2-methylpropane-2- sulfinamide (formula 19) with an acid and a reducing agent. (S)-N-(5-((R)-2-(2,5-difluorophenyl)-pyrrolidin-l-yl)-pyrazolo[l,5- a]pyrimidin-3-yl)-3-hydroxypyrrolidine-l-carboxamide, is a tyrosin kinase (TRK) inhibitor for trearing e.g. cancer.
    • 制备(S)-N-(5 - ((R)-2-(2,5-二氟苯基)吡咯烷-1-基)吡唑并[1,5-a]嘧啶-4 (5 - ((R)-2-(2,5-二氟苯基)吡咯烷-1-基)-3,3a(三唑-3-基)-3-羟基吡咯烷-1-甲酰胺(式I)或其盐 - 二氢吡唑并[1,5-a]嘧啶-3-基)氨基甲酸叔丁酯或类似衍生物(式13)与(S) - 吡咯烷-3-醇(式14) (5 - ((R)-2-(2,5-二氟苯基)吡咯烷-1-基)-3,3a-二氢吡唑并[1,5-a]嘧啶-3-基)氨基甲酸酯(式13 )或(R)-5-(2-(2,5-二氟苯基)吡咯烷-1-基)-3-硝基吡唑并[1,5-a]嘧啶(式11)还原成(R) -5-(2-(2,5-二氟苯基)吡咯烷-1-基)吡唑并[1,5-a]嘧啶-3-胺(式12)。 通过处理(R)-N - ((R)-1-(2,5-二氟苯基)吡咯烷(R)-2-羟基琥珀酸盐(式10) -3-(1,3-二恶烷-2-基)丙基)-2-甲基丙烷-2-亚磺酰胺(式19)与酸和还原剂反应。 (S)-N-(5 - ((R)-2-(2,5-二氟苯基) - 吡咯烷-1-基) - 吡唑并[1,5-a]嘧啶-3-基)-3-羟基吡咯烷-3-甲酸 1-甲酰胺是酪氨酸激酶(TRK)抑制剂,用于处理例如, 癌症