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    • 16. 发明公开
    • 터비나핀 및 그의 염산염 제조방법
    • 通过使用具有高成像率和高纯度的高分子量的氯离子中间体生产酪氨酸及其盐酸盐的方法
    • KR1020050004925A
    • 2005-01-13
    • KR1020030042553
    • 2003-06-27
    • 주식회사 코오롱
    • 채희성김상호김윤철박호진
    • C07C209/06
    • PURPOSE: Provided is a method for producing terbinafine and its hydrochloride useful for fungal squalene epoxidase inhibitor, which improves selectivity to a stereo-isomer, yield and purity without using any expensive materials. CONSTITUTION: The method for producing terbinafine comprises the steps of: (a) reacting 6,6-dimethyl-1-heptene-4-ynyl-3-alcohol represented by the following formula 3 with a chlorinating agent to form a chloride intermediate represented by the following formula 4; and (b) coupling the chloride intermediate represented by formula 4 with N-methyl-1-naphthalenemethaneamine represented by the following formula 5 in the presence of potassium carbonate as a base to form (e)-N-(6,6-dimethyl-2-heptyn-4-ynyl)-N-methyl-1-naphthaleneamine(terbinafine) represented by the following formula 1.
    • 目的:提供特比萘芬及其盐酸盐可用于真菌角鲨烯环氧化物酶抑制剂的方法,该方法提高了立体异构体的选择性,产率和纯度,而无需使用任何昂贵的材料。 构成:特比萘芬的制造方法包括以下步骤:(a)将由下式3表示的6,6-二甲基-1-庚烯-4-炔基-3-醇与氯化剂反应,形成由 以下公式4; 和(b)将由式4表示的氯化物中间体与由下式5表示的N-甲基-1-萘甲烷胺在碳酸钾作为碱的存在下偶合形成(e)-N-(6,6-二甲基 - 2-庚炔-4-炔基)-N-甲基-1-萘胺(特比萘芬)。