S type 2-substituted hydroxy-2-indolidinylbutyric ester...

C - Chemistry – Metallurgy – 07 – D

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C07D 491/22 (2006.01) C07D 209/42 (2006.01) C07D 217/26 (2006.01) C07D 491/14 (2006.01) C07D 491/147 (2006.01) C07D 491/20 (2006.01)

Patent

CA 2219692

The present invention is directed to a process for preparing S type 2- substituted hydroxy-2-indolidinylbutyric ester compound [II]: (see formula) wherein R0 is a residue of nitrogen-containing fused heterocyclic carboxylic acid having absolute configuration of "R" (in which the nitrogen atom is protected), R1 and R2 are lower alkyl groups, and E is an ester residue. The compound of the present invention is useful as an intermediate for preparing camptothecin derivatives having antitumor activities, which comprises 2-ethylating 2- substituted hydroxy-2-indolidinylacetic ester compound [I]: (see formula ) wherein R0, R1, R2 and E are as defined above.

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