C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 413/12 (2006.01) C07D 233/54 (2006.01) C07D 233/64 (2006.01) C07D 401/12 (2006.01) C07D 403/12 (2006.01) C07D 417/12 (2006.01)
Patent
CA 2139362
A novel synthetic intermediate (II) useful for preparation of compound (I) possessing renin-inhibitory activity, and processes for preparing the compound (I) using said intermediate (II), which is schematically shown in the following: Image + Image (II) (III) Elimination of the Image N-protective group if necessary (I) wherein R1 is lower alkyl which may be substituted by a group of the formula -N(R7)-CO-N(R8)(R9) (wherein R7 is hydrogen or lower alkyl, and R8 and R9 together with the attached nitrogen atom form a heterocyclic group optionally substituted), or the like; R2 is hydrogen, lower alkyl, or the like; R3 is hydrogen or lower alkyl; R4 is hydrogen or an N-protective group; R5 is hydrogen or a carboxy-protective group; and R10 is lower alkyl. The process via the intermediate (II) of the present invention is industrially advantageous in that it affords the final product (I) at high yields from cheaper starting materials as compared with the conventional methods, and that a remarkable reduction of preparation cost can be achieved.
Furutera Tetsuo
Kagara Kooji
Kawai Nobutaka
Machiya Koji
Nakamura Takashi
Fujisawa Pharmaceutical Co. Ltd.
Swabey Ogilvy Renault
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