AI Article Synopsis
- A new method using mild palladium catalysis has been developed to synthesize the hormone calcitriol and its analogues.
- This technique involves a one-pot reaction at room temperature with two steps: first, a palladium-catalyzed cyclization, followed by a Negishi cross-coupling with alkenyl zinc.
- This approach allows for the creation of various new vitamin D analogues that could have therapeutic applications, especially with changes to specific parts of the molecule.
Article Abstract
[reaction: see text] A mild palladium-catalyzed cascade has been used for the synthesis of the hormone 1alpha,25-dihydroxyvitamin D3 (calcitriol, 1a) and its analogues 1b and 1c. This one-pot process involves two consecutive transformations at room temperature: An initial palladium-catalyzed 6-exo-cyclocarbopalladation of vinyl triflates followed by a Negishi cross-coupling reaction with an alkenyl zinc. This novel strategy opens new possibilities for the preparation of a variety of new vitamin D analogues of therapeutic potential, particularly with modifications at the triene and/or ring-A.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1021/ol052489c | DOI Listing |
Publication Analysis
Top Keywords
pd-catalyzed carbocyclization-negishi
4
carbocyclization-negishi cross-coupling
4
cross-coupling cascade
4
cascade novel
4
novel approach
4
approach 1alpha25-dihydroxyvitamin
4
1alpha25-dihydroxyvitamin analogues
4
analogues [reaction
4
[reaction text]
4
text] mild
4
Similar Publications
Want AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!