PROBLEM TO BE SOLVED: To provide a simple and industrially advantageous method for producing an amine derivative having activity to inhibit amyloid &beta protein secretion and cumulation.SOLUTION: This method for producing in high yield and quality an amine derivative V having the activity to inhibit amyloid &beta protein secretion and deposition involves splitting no amido linkage in a compound I but selectively splitting only the ether linkage in the compound I without causing the tertiary amine to be converted to the corresponding quaternary salt [R is a hydrocarbon group R1 and R2 are each H or a 1-6C alkyl, or may form a nitrogen-containing heterocyclic ring together with the adjoining nitrogen atom ring A a benzene ring ring B is a 4 to 8-membered ring Y is a bivalent 1-6C aliphatic hydrocarbon group X is a hydrocarbon group or cyclic group and L is an eliminable group or hydroxyl group].COPYRIGHT: (C)2001,JPO(修正有)【課題】 アミロイドβ蛋白分泌、蓄積阻害作用を有するアミン誘導体の簡便で工業的に有利な製造法を提供する。【解決手段】[Rは炭化水素基を示し、R1およひR2は水素またはC1-6アルキル基を示すか、または隣接する窒素と共に含窒素複素環を形成してもよく、A環はベンゼン環を、B環は4~8員環を、Yは2価のC1-6脂肪族炭化水素基を示す。Xは炭化水素基または環状基を、Lは脱離基または水酸基を示す。]化合物Iの同一分子内に存在するアミド結合を切断せずエーテル結合のみを選択的に切断し、また3級アミンの4級塩化が起こらないため、アミロイドβ蛋白分泌、蓄積阻害作用を有するアミン誘導体Vを高収率、高品質で得る製造法。
