Ghosh, Arun K.; Allu, Srinivasa Rao; Reddy, Guddeti Chandrashekar; Lopez, Adriana Gamboa; Mendez, Patricia; Jurica, Melissa S. published an article in 2021, the title of the article was Design and synthesis of herboxidiene derivatives that potently inhibit in vitro splicing.Synthetic Route of 2873-29-2 And the article contains the following content:
Herboxidiene is a potent antitumor agent that targets the SF3B subunit of the spliceosome. Herboxidiene possesses a complex structural architecture with nine stereocenters and design of potent less complex structures would be of interest as a drug lead as well as a tool for studying SF3B1 function in splicing. We investigated a number of C-6 modified herboxidiene derivatives in an effort to eliminate this stereocenter and, also to understand the importance of this functionality. The syntheses of structural variants involved a Suzuki-Miyaura cross-coupling reaction as the key step. The functionalized THF core has been constructed from com. available optically active tri-O-acetyl-D-glucal. We investigated the effect of these derivatives on splicing chem. The C-6 alkene derivative showed very potent splicing inhibitory activity similar to herboxidiene. Furthermore, the C-6 gem-di-Me derivative also exhibited very potent in vitro splicing inhibitory activity comparable to herboxidiene. The experimental process involved the reaction of (2R,3S,4R)-2-(Acetoxymethyl)-3,4-dihydro-2H-pyran-3,4-diyl diacetate(cas: 2873-29-2).Synthetic Route of 2873-29-2
The Article related to herboxidiene derivative preparation splicing inhibitor suzuki miyaura cross coupling, Heterocyclic Compounds (One Hetero Atom): Pyrans and other aspects.Synthetic Route of 2873-29-2
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