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• W1972571586 abstract "Recently we created the novel indolylprodigiosin derivative 2 (obatoclax) and demonstrated its ability to antagonize multiple members of the B-cell lymphoma (Bcl) family of antiapoptotic proteins. The compound has shown potent anticancer activity in several animal tumor models. Obatoclax is now in Phase 1b and 2 clinical trials directed against multiple hematologic and solid tumor malignancies. To support its clinical development, a new scalable synthesis was required. Obatoclax has been prepared using a three-step synthesis, starting from commercially available 4-methoxy-3-pyrrolin-2-one. The reaction sequence involves a haloformylation reaction followed by a Suzuki cross-coupling reaction with an indole-2-boronic acid. The synthesis is completed by an acid-mediated condensation with 2,4-dimethyl-1H-pyrrole." @default.
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• W1972571586 date "2007-11-01" @default.
• W1972571586 modified "2023-10-16" @default.
• W1972571586 title "A Scalable Process for the Synthesis of the Bcl Inhibitor Obatoclax" @default.
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• W1972571586 doi "https://doi.org/10.1021/op7001613" @default.
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