Highly stereoselective trifluoropyruvate-ene reaction with Δ20(22)-steroidal olefin by chiral Pd2+-catalyst: New type of VDR antagonist for osteocalcin, Δ20(21)-ene product without (dehydro)lactone and lactam motifs
Publication date: March 2019
Source: Journal of Fluorine Chemistry, Volume 219
Author(s): Kumiko Fujita, Koichi Mikami
The highly stereoselective trifluoropyruvate-ene reaction with steroidal 1,1-disubstituted Δ20(22)-side chain olefin was achieved by the dicationic BINAP-Pd complex as an effective chiral Lewis acid catalyst to give the Δ20(21)-steroidal ene-product in high yield and enantioselectivity. The ene product itself without (dehydro)lactone and lactam structures exhibited remarkably high antagonist activity for human osteocalcin even in low binding affinity for human vitamin D hormone receptor.
Keeping up-to-date with research can feel impossible, with papers being published faster than you'll ever be able to read them. That's where Researcher comes in: we're simplifying discovery and making important discussions happen. With over 19,000 sources, including peer-reviewed journals, preprints, blogs, universities, podcasts and Live events across 10 research areas, you'll never miss what's important to you. It's like social media, but better. Oh, and we should mention - it's free.
Researcher displays publicly available abstracts and doesn’t host any full article content. If the content is open access, we will direct clicks from the abstracts to the publisher website and display the PDF copy on our platform. Clicks to view the full text will be directed to the publisher website, where only users with subscriptions or access through their institution are able to view the full article.