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    • 10. 发明授权
    • Stereoselective synthesis of certain trifluoromethyl-substituted alcohols
    • 某些三氟甲基取代的醇的立体选择性合成
    • US07256300B2
    • 2007-08-14
    • US11081063
    • 2005-03-15
    • Thomas Wai-Ho LeeJohn Robert Proudfoot
    • Thomas Wai-Ho LeeJohn Robert Proudfoot
    • C07D301/02
    • C07D303/22C07D301/02C07D303/08C07D407/06
    • A process for stereoselective synthesis of a compound of Formula (X) or Formula (X′) wherein R1, R2, and R3 are as defined herein, the process comprising: (a) reacting the starting material of formula A with a chiral sulfoxide anion source in a suitable solvent to prepare a compound of formula C or C′; (b) reducing the sulfoxide of formula C or C′ in a suitable solvent to obtain the compound of formula D or D′; and (c) cyclizing the compound of formula D or D′ in a suitable solvent to form the epoxide compound of Formula (X) or Formula (X′), or a tautomer, prodrug, solvate, or salt thereof; pharmaceutical compositions containing such compounds, and methods of modulating the glucocorticoid receptor function and methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammatory, allergic, or proliferative processes in a patient using these compounds.
    • 用于立体选择性合成式(X)或式(X')的化合物的方法,其中R 1,R 2和R 3, 所述方法包括:(a)使式A的原料与手性亚砜阴离子源在合适的溶剂中反应以制备式C或C'的化合物; (b)在合适的溶剂中还原式C或C'的亚砜,得到式D或D'的化合物; 和(c)在合适的溶剂中使式D或D'化合物环化以形成式(X)或式(X')的环氧化合物或其互变异构体,前药,溶剂合物或盐; 含有这些化合物的药物组合物,以及调节糖皮质激素受体功能的方法和治疗由糖皮质激素受体功能介导的疾病状态或病症的方法,或其特征在于使用这些化合物的患者的炎症,过敏或增殖过程。