| 摘要 |
PROBLEM TO BE SOLVED: To produce a new azaspiro compound capable of being derivatized into azaspiranes useful as an immunosumppressant in a short process. SOLUTION: This compound is represented by formula I [R1 is H, a 1-12C alkyl, a 2-12C alkenyl or the like; R2 and R3 are each H, a 1-12C alkyl, a (substituted)aryl or the like; R4 and R5 are each a 1-12C alkyl, a (substituted) aralkyl or the like; (x) is 0 or 1; (y) is 2-5; (z) is 0-6], e.g. 2-[3-(N,N-diethylamino) propyl]-7,9-dimethoxy-2-azaspiro[4.5]deca-6,9-dien-1-one. The compound represented by formula I is produced by reacting a compound represented by formula II (R6 is OH, a 1-12C alkoxy or the like) e.g. 3,5-dimethoxybenzoic acid) with a compound represented by the formula X(CH2)yY (X is a halogen; Y is an alkanesulfonyloxy or the like) (e.g. 1,2-dibromoethane) in the presence of an alkali metal and alcohols in liquid ammonia, providing a compound represented by formula III and then reacting the resultant compound represented by formula III with a compound represented by the formula R1(CH2)zNH2.
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