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    • 4. 发明申请
    • PROCESS FOR THE SYNTHESIS OF N- [3-(3-CYANOPYRAZOLO [1,5A] PYRIMIDIN-7-YL)-PHENYL]-N-ETHYL-ACETAMIDE
    • 合成N- [3-(3-氰基吡唑并[1,5A]吡啶基-7-YL) - 苯基] -N-乙基 - 乙酰胺的方法
    • WO2005073235A2
    • 2005-08-11
    • PCT/HU2005/000008
    • 2005-01-31
    • RICHTER GEDEON VEGYÉSZETI GYÁR RT.CZIBULA, LászlóDOBAY, LászlóSZÕKE, KatalinWERKNÉ PAPP, ÉvaNAGYNÉ BAGDY, JuditTÁRKÁNYI, Gábor
    • CZIBULA, LászlóDOBAY, LászlóSZÕKE, KatalinWERKNÉ PAPP, ÉvaNAGYNÉ BAGDY, JuditTÁRKÁNYI, Gábor
    • C07D487/04
    • C07D487/04C07C233/43
    • The invention relates to N- [3- (3-cyanopyrazolo [1,5-a] pyrimidin-7-yl) - phenyl]-N-ethyl-acetamide of formula (IV) containing less than 0.2 % impurities, which is suitable for therapeutic application. Furthermore the invention relates to a process for the synthesis of therapeutically applicable compound of formula (IV) containing less than 0.2 % impurities by reacting the new intermediate N-{3-[3-(dimethylamino)-1-oxo-2-propenyl]phenyl}-N-ethyl­acetamide hydrochloride of formula (II) and 3-amino-4-pyrazol-carbonitrile base of formula (III) in an acid free medium. The invention also relates to the new N- {3- [3- (dimethylamino) -1- oxo -2- ­propenyl]phenyl } -N-ethyl-acetamide hydrochloride of formula (II). The invention also relates to a process for the synthesis of the new N- [3- [3, (dimethylamino)-1-oxo-2-propenyl]phenyl}-N-ethyl-acetamide hydrochloride of formula (II) having a purity of more than 99.5 %. Furthermore the invention relates to N-{3-[3-cyanopyrazolo (1,5-a) pyrimidin]­6 -yl-3- [ (3-N-ethyl-acetamido-phenyl) -3-oxo-propen-1-yl] - (pyrimidin-7-yl) -phenyl} - N-ethyl-acet-amide of formula (V), which is an isolated new impurity formed in 0.07 % yield during the synthesis of compound of formula (IV).
    • 本发明涉及含有小于0.2%杂质的式(IV)的N- [3-(3-氰基吡唑并[1,5-a]嘧啶-7-基) - 苯基] -N-乙基 - 乙酰胺,其是合适的 用于治疗应用。 此外,本发明涉及通过使新的中间体N- {3- [3-(二甲基氨基)-1-氧代-2-丙烯基] -1-哌嗪基] 苯基} -N-乙基乙酰胺盐酸盐和式(III)的3-氨基-4-吡唑基 - 腈基的无酸介质中。 本发明还涉及式(II)的新的N- {3- [3-(二甲基氨基)-1-氧代-2-丙烯基]苯基} -N-乙基 - 乙酰胺盐酸盐。 本发明还涉及合成具有纯度的式(II)的新的N- [3- [3,(二甲基氨基)-1-氧代-2-丙烯基]苯基} -N-乙基 - 乙酰胺盐酸盐的方法 超过99.5%。 此外,本发明涉及N- {3- [3-氰基吡唑并(1,5-a)嘧啶] -6-基-3 - [(3-N-乙基 - 乙酰氨基 - 苯基)-3-氧代 - 吡啶-2-基] - (嘧啶-7-基) - 苯基} -N-乙基 - 乙酰胺,其是在合成式(IV)化合物期间以0.07%产率形成的分离的新杂质。