发明名称 Methods for producing cyclic benzamidine derivatives
摘要 In the present invention, the methods of producing a fluorinated cyclic benzamidine derivative (A), or a salt thereof, comprise the step of reacting a specific novel compound with ammonia or imide. The methods of this invention for producing a morpholine-substituted phenacyl derivative (B), or a salt thereof, comprise reaction of a specific novel compound with morpholine, reaction of the product with a halogenating reagent, and deketalization of the product. The methods of this invention for a producing cyclic benzamidine derivative (C), or a salt thereof, comprise the step of coupling compound (A), or a salt thereof, with compound (B), or a salt thereof, in the presence of an ether or a hydrocarbon. The methods of this invention for recrystallizing a cyclic benzamidine derivative (C), or a salt thereof, comprise the steps of dissolving compound (C), or the salt thereof, in a mixed solvent comprising an alcohol and water, or a mixed solvent comprising an ether and water, and after dissolution, adding additional water to precipitate crystals of compound (C), or the salt thereof.
申请公布号 US2006058370(A1) 申请公布日期 2006.03.16
申请号 US20050208289 申请日期 2005.08.18
申请人 EISAI CO., LTD. 发明人 SHIMOMURA NAOYUKI;SASHO MANABU;KAYANO AKIO;YOSHIZAWA KAZUHIRO;TSUJII MASAHIKO;KURODA HIROSHI;FURUKAWA KEN
分类号 C07D209/44;A61K31/4035 主分类号 C07D209/44
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