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    • 5. 发明公开
    • 발사르탄의 제조 방법 및 이에 사용되는 신규 중간체
    • 制备过程中使用的VALSARTAN和新型中间体的方法
    • KR1020110089671A
    • 2011-08-09
    • KR1020100009168
    • 2010-02-01
    • 경동제약 주식회사
    • 이병석신상훈안유길
    • C07D257/04A61K31/41A61P9/12
    • PURPOSE: A method for preparing valsartan and a novel intermediate for the same are provided to develop a therapeutic agent for treating hypertension or cardiac failure. CONSTITUTION: A method for preparing valsartan comprises: a step of reacting L-valine amide of formula VI or hydrochloride thereof with a compound of formula VII under the presence of base and selective catalyst to prepare a L-valine amide derivative of formula IV or salt thereof; a step of reacting the L-valien amide derivative of formula IV or salt thereof with N-pentanoyl chloride of formula V in a reaction solvent under the presence of base to prepare a L-valine amide derivative of formula III; a step of trityl group in the compound of formula III in a reaction solvent under the presence of selective acid to prepare a L-valine amide derivative of formula II; and a step of hydrolyzing the L-valine amide derivative of formula II.
    • 目的:提供一种制备缬沙坦及其新型中间体的方法,以开发治疗高血压或心力衰竭的治疗剂。 构成:制备缬沙坦的方法包括:在碱和选择性催化剂的存在下使式Ⅵ或其盐酸盐的L-缬氨酸酰胺与式Ⅶ化合物反应以制备式Ⅳ的L-缬氨酸酰胺衍生物或盐 物; 在反应溶剂中,在碱的存在下,使式Ⅳ的L-缬氨酰胺衍生物或其盐与式Ⅴ的N-戊酰氯反应以制备式Ⅳ的缬氨酸酰胺衍生物的步骤; 在反应溶剂中,在选择性酸的存在下,式III化合物中的三苯甲基的步骤,以制备式Ⅱ的L-缬氨酸酰胺衍生物; 和水解式Ⅱ的L-缬氨酸酰胺衍生物的步骤。