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Ti(II) and Rh(I) Complexes as Reagents towards Thapsigargin Core.

08:00 EDT 9th April 2019 | BioPortfolio

Summary of "Ti(II) and Rh(I) Complexes as Reagents towards Thapsigargin Core."

A novel approach towards the [5-7] fused bicyclic core of thapsigargin, a subnanomolar inhibitor of the endo/sarcoplasmic calcium ATPase (SERCA), is presented. The synthetic route includes an original Ti(II)-mediated hydroxy-directed reductive coupling of an enantiomerically enriched propargylic alcohol and an intramolecular Rh(I)-catalyzed cyclocarbonylation reaction as key steps. Interestingly, through first experiments of titanocene-mediated reductive cyclization of a 1,8-enyne, a seven-membered cycle was isolated as a unique product with a total diastereoselectivity.

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This article was published in the following journal.

Name: The Journal of organic chemistry
ISSN: 1520-6904
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