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1. Development and Scale-up of a Flow Chemistry Lithiation–Borylation Route to a Key Boronic Acid Starting Material

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   Contributor(s):: Usutani, Hirotsugu, Nihei, Takashi, Papageorgiou, Charles D., Cork, David G.

   A flow chemistry process for the synthesis of a key boronic acid starting material was developed utilizing flow flash chemistry that allowed formation and subsequent productive reaction of an unstable organolithium intermediate. Rapid scale-up from Discovery Chemistry and process optimization to...

2. Application of Continuous Flow for DIBAL-H Reduction and n-BuLi Mediated Coupling Reaction in the Synthesis of Eribulin Mesylate

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   Contributor(s):: Fukuyama, Takashi, Chiba, Hiroyuki, Kuroda, Hirofumi, Takigawa, Teiji, Kayano, Akio, Tagami, Katsuya

   Here we examined the use of continuous flow conditions for the final assembly of eribulin mesylate aimed to avoid cryogenic condition. The diisobutylaluminum hydride reduction of ester 2 to aldehyde 3 and n-butyllithium-mediated coupling of aldehyde 3 and sulfone fragment 4 to produce...