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    • 2. 发明申请
    • A PROCESS FOR THE PREPARATION OF 5-(HALOACETYL)-8-(SUBSTITUTED OXY)-(1H)-QUINOLIN-2-ONES
    • 制备5-(HALOACETYL)-8-(取代的氧) - (1H) - 喹啉-2-酮的方法
    • WO2004087668A1
    • 2004-10-14
    • PCT/EP2004/003479
    • 2004-04-01
    • NOVARTIS AGNOVARTIS PHARMA GMBHLOHSE, OlivierPENN, GerhardSCHILLING, Hanspeter
    • LOHSE, OlivierPENN, GerhardSCHILLING, Hanspeter
    • C07D215/26
    • C07D215/26Y02P20/55
    • The invention relates to a process for preparing 5-(α-haloacetyl)-8-substituted oxy-( 1H )-quinolin-2-ones. The process involves (i) reacting (a) 8-hydroxy-( 1H )-quinolin-2-one with an acylating agent and a Lewis acid to form 5-acetyl-8-hydroxy-( 1H )-quinolin-2-one; or (b) 8-hydroxy-( lH )-quinolin-2-one with an acylating agent to form 8-acetoxy-( lH )-quinolin-2-one, and treating, in-situ, the 8-acetoxy-( 1H )-quinolin-2-one with a Lewis acid to form 5-acetyl-8-hydroxy-( 1H )-quinolin-2-one; or (c) 8-acetoxy-( 1H )-quinolin-2-one with a Lewis acid to form 5-acetyl-8-hydroxy-( lH )-quinolin-2-one; (ii) reacting the 5-acetyl-8-hydroxy-( 1H )-quinolin-2-one prepared in Step (i) with a compound having the Formula RL in the presence of a base and a solvent to form 5-acetyl-8-substituted oxy-( 1H )-quinolin-2-one, wherein R is a protecting group and L is a leaving group; and (iii) reacting the 5-acetyl-8-substituted oxy-( 1H )-quinolin-2-one with a halogenating agent in the presence of a solvent to form a 5-(α-haloacetyl)-8-substituted oxy-( 1H )-quinolin-2-one.
    • 本发明涉及制备5-(α-卤代乙酰基)-8-取代的氧基 - (1H) - 喹啉-2-酮的方法。 该方法包括(i)使(a)8-羟基 - (1H) - 喹啉-2-酮与酰化剂和路易斯酸反应,形成5-乙酰基-8-羟基 - (1H) - 喹啉-2-酮 ; 或(b)8-羟基 - (1H) - 喹啉-2-酮与酰化剂反应形成8-乙酰氧基 - (1H) - 喹啉-2-酮,并原位处理8-乙酰氧基 - ( 1H) - 喹啉-2-酮与路易斯酸形成5-乙酰基-8-羟基 - (1H) - 喹啉-2-酮; 或(c)8-乙酰氧基 - (1H) - 喹啉-2-酮与路易斯酸形成5-乙酰基-8-羟基 - (1H) - 喹啉-2-酮; (ii)使步骤(i)中制备的5-乙酰基-8-羟基 - (1H) - 喹啉-2-酮与碱式和溶剂存在下的具有式RL的化合物反应,形成5-乙酰基 - 8-取代的氧 - (1H) - 喹啉-2-酮,其中R是保护基,L是离去基团; 和(iii)使5-乙酰基-8-取代的氧基 - (1H) - 喹啉-2-酮与卤化剂在溶剂存在下反应,形成5-(α-卤代乙酰基)-8-取代的氧 - (1H) - 喹啉-2-酮。