Guan-Hua Wang, Hu-Shan Zhang, Jing Zhou
Aug 1, 2008
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Influential Citations
7
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Synthesis
Abstract
ABT-263, a newly developed Bcl-2 inhibitor, was efficiently synthesized. The key intermediates 4-(4-{[2-(4-chlorophenyl)-5,5-dimethylcyclohex-1-enyl]methyl}piperazin-1-yl)benzoic acid and 4-fluoro-3-[(trifluoromethyl)sulfonyl]benzenesulfonamide were efficiently prepared by a three-component Mannich reaction and by nucleophilic fluorination of 1-nitro-2-[(trifluoromethyl)sulfonyl]benzene as the key steps, respectively. Our work may lay a foundation for a new process development of this promising anticancer drug candidate.