会员体验
专利管家(专利管理)
工作空间(专利管理)
风险监控(情报监控)
数据分析(专利分析)
侵权分析(诉讼无效)
联系我们
交流群
官方交流:
QQ群: 891211   
微信请扫码    >>>
现在联系顾问~
热词
    • 10. 发明授权
    • Process for the preparation of (S)-alpha-ethyl-2-oxo-1-pyrrolidineacetamide and (R)-alpha-ethyl-2-oxo-pyrrolidineacetamide
    • 制备(S)-α-乙基-2-氧代-1-吡咯烷乙酰胺和(R)-α-乙基-2-氧代 - 吡咯烷乙酰胺的方法
    • US07902380B2
    • 2011-03-08
    • US11667824
    • 2005-11-21
    • Yuan Qiang LiZhi-Xian WangBhaskar Reddy Guntoori
    • Yuan Qiang LiZhi-Xian WangBhaskar Reddy Guntoori
    • C07D207/12
    • C07D207/27
    • A process provided for the preparation of the (S)- and (R)- alpha- ethyl-2-oxo-1-pyrrolidineacetamide of formula:(1) from (RS)-alpha-ethyl-2-oxo-1-pyrrolidineacetic acid of formula:(2) comprising: i) combining the (RS)-2 with a chiral base (resolving agent) in a resolution solvent and crystallizing from the said mixture the diastereomeric salt of (S)- or (R)-2 and chiral base; ii) regenerating (S)- or (R)-2 from the crystallized diastereomeric salt by treating with a suitable acid or acidic ion-exchange resin; iii) optionally regenerating (R)- or (S)-2 or their mixture (predominantly one enantiomer) from the crystallization mother liquor by treating with a suitable acid or acidic ion-exchange resin; iv) optionally epimerizing (RS)-2 by treating (R)- or (S)-2 or their mixture (predominantly one enantiomer) of step iii with an acid anhydride; V) optionally converting (RS)-2 of step iv into enantiomerically enriched (S)- or (R)-2 through steps i and ii; vi) formation of the mixed anhydride by reacting (R)- or (S)-2 with an alkyl or aryl sulfonyl halogen compound RSO2X in the presence of a suitable base; and vii) reacting the mixed anhydride with ammonia; wherein R represents C 1 to C 15 alkyl or aryl groups such as methyl, ethyl, p-toluenyl, 2,4,6-trimethylbenzyl, 2,4,6-trichloribenzyl, and X represents a halogen atom such as F, Cl and Br atoms.
    • 由(RS)-α-乙基-2-氧代-1-吡咯烷乙酸制备式(1)的(S) - 和(R)-α-乙基-2-氧代-1-吡咯烷乙酰胺的方法 式(2)的酸包括:i)将(RS)-2与分解溶剂中的手性碱(拆分剂)组合并从所述混合物中结晶出(S) - 或(R)-2的非对映体盐 和手性基; ii)通过用合适的酸或酸性离子交换树脂处理从结晶的非对映体盐再生(S) - 或(R)-2) iii)通过用合适的酸或酸性离子交换树脂处理任选地从结晶母液中再生(R) - 或(S)-2或它们的混合物(主要是一种对映异构体) iv)通过用酸酐处理(R) - 或(S)-2或它们的步骤iii的混合物(主要是一个对映异构体)任选差向异构化(RS)-2; V)任选地通过步骤i和ii将步骤iv的(RS)-2转化成对映异构体富集的(S) - 或(R) vi)通过使(R) - 或(S)-2与烷基或芳基磺酰基卤化合物RSO 2 X在合适的碱的存在下反应形成混合酸酐; 和vii)使混合酸酐与氨反应; 其中R表示C 1至C 15烷基或芳基如甲基,乙基,对甲苯基,2,4,6-三甲基苄基,2,4,6-三氯苄基,X表示卤素原子如F,Cl和 Br原子。