UC Santa Cruz
Total synthesis of GEX1Q1, assignment of C-5 stereoconfiguration and evaluation of spliceosome inhibitory activity
- Author(s): Ghosh, AK
- Ma, N
- Effenberger, KA
- Jurica, MS
- et al.
Published Web Locationhttp://www.ncbi.nlm.nih.gov/pmc/articles/PMC4051430/
An enantioselective total synthesis of GEX1Q1 has been accomplished in a convergent manner. The C-5 asymmetric center has now been assigned through synthesis. GEX1Q1 displayed slightly better spliceosome inhibitory activity over its C-5 epimer. The salient features of this synthesis include an asymmetric hetero-Diels-Alder reaction to construct the tetrahydropyran ring and a Suzuki cross-coupling to assemble the key segments. © 2014 American Chemical Society.
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