| 摘要 |
PROBLEM TO BE SOLVED: To produce new azaspirodiones capable of being derivatized into azaspiranes useful as an immunosuppressant in a short process. SOLUTION: The compounds are 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 1-12 C alkyl, a (substituted)aryl or the like; R4 and R5 are each a 1-12C alkyl, a (substituted) alkyl or the like; (x) is 0 or 1; (y) is 2-5; (z) is 0-6], e.g. 2-[3-(N,N-dimethylamino) propyl]-2-azaspiro[4.5]decan-7,9-dione. The compounds represented by formula I are obtained by reducing a compound represented by formula II (R6 and R7 are each a 1-12C alkyl, a 2-12C alkenyl or the like) e.g. 2-(3-aminopropyl)-7,9- dimethoxy-8,8-di-n-propyl-2-azaspiro[4.5]deca-6,9-dien-1-one} with a reducing agent such as preferably lithium aluminum hydride, providing a compound represented by formula III and then treating the resultant compound represented by formula III with an acid.
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