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    • 4. 发明公开
    • 신규 결정형 에스잘토프로펜 및 그의 제조방법
    • 新型结晶S-ZALTOPROFEN,其制备方法
    • KR1020130063183A
    • 2013-06-14
    • KR1020110129567
    • 2011-12-06
    • 대화제약 주식회사
    • 이한구박웅재권오설조영우박영택
    • C07D337/14A61K31/38A61P19/02
    • PURPOSE: A method for preparing novel crystalline S-zaltoprofen is provided to obtain high purify and high yield S-zaltoprofen, and to use S-zaltoprofen as an analgesic agent for chronic rheumatoid arthritis and osteoarthrosis. CONSTITUTION: Crystalline S-zaltoprofen of chemical formula 2 has 99% ee or more of optical purity. The crystalline S-zaltoprofen has an X-ray powder diffraction peak at 6.62, 6.99, 9.59, 9.75, 14.06, 14.98, 15.20, 15.48, 15.70, 19.27, 19.64, 20.81, 21.19, 21.51, 22.13, 22.56, 23.63, 24.33, 24.62, 24.93, 25.36, 26.21, 26.46, 26.91, 27.28, 28.23, 28.42, 29.11, and 34.23 2θ (+/- 0.2). A method for preparing S-zaltoprofen in a mixture solvent containing water and an organic solvent comprises: a step of reacting racemic zaltoprofen of chemical formula 1 with chiral amine in an organic solvent, and isolating S-zaltoprofen-chiral amine; a step of treating S-zaltoprofen-chiral amine with acid and isolating S-zaltoprofen; and a step of preparing S-zaltoprofen in the mixture solvent of water and the organic solvent.
    • 目的:提供一种制备新型结晶S-扎洛芬的方法,以获得高纯度和高产量的S-扎洛芬,并使用S-扎洛芬作为慢性类风湿性关节炎和骨关节炎的止痛剂。 构成:化学式2的结晶S-扎洛芬具有99%ee以上的光学纯度。 结晶S-扎洛芬在6.62,6.99,9.99,9.75,14.06,14.98,15.20,15.48,15.70,19.27,19.64,20.81,21.19,21.51,22.13,22.56,23.63,24.33, 24.62,24.93,25.36,26.21,26.46,26.91,27.28,28.23,28.42,29.11和34.23 2& (+/- 0.2)。 在含水和有机溶剂的混合溶剂中制备S-扎洛芬的方法包括:将化学式1的外消旋的扎洛芬与手性胺反应在有机溶剂中并分离S-噻洛芬手性胺的步骤; 用酸处理西扎洛芬 - 手性胺并分离S-zaltoprofen的步骤; 以及在水和有机溶剂的混合溶剂中制备S-扎洛芬的步骤。