Process for the preparation of substituted indolinone...

Details Process for the preparation of substituted indolinone... Process for the preparation of substituted indolinone...

C - Chemistry, Metallurgy

07

D

260/320

C07D 209/34 (2006.01)

Patent

CA 1305711

11927 ABSTRACT A process for the preparation of a compound of structure (I) Image (I) in which, each group R is hydrogen, C1-6alkyl, C3-6allyl, phenylC1-6alkyl or 4-hydroxyphenylC1-6alkyl; R1, R2 and R3 are hydrogen or C1-6alkyl; R4 is hydrogen or hydroxy; and n is 1 to 3 or a pharmaceutically acceptable salt thereof, which comprises reduction of a compound of structure (II) Image (II) in which R, R2 to R4 and n are as described above and R5 is hydrogen or a cation, followed by cyclisation of the intermediate so formed. and, optionally, alkylating to form a compound of structure (I) in which R1 is C1-6- alkyl and, optionally, forming a pharmaceutically acceptable salt thereof, characterised in that the reduction of the compound of structure (II) is carried out by catalytic transfer hydrogenation in water as a solvent.

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