A novel aerobic manganese-catalyzed oxophoshporylation reaction of carbon–carbon double bonds of styrene derivatives and vinyl ethers using diethyl H-phosphonates was developed. This direct transformation of alkenes to b-ketophosphonates readily proceeded at room temperature via the incorporation of molecular oxygen present in air (open flask). All of the experimental procedures in this reaction can be performed in air without cooling, heating, or high pressure. This methodology serves an alternative approach to produce β-ketophosphonates because of its simplicity and mildness.
4-epi-Jaspine B derivatives containing a polar functional group in the lipid tail were designed and synthesized for the development of sphingosine kinase (SphK) inhibitors, which would be applicable to the treatment of autoimmune and inflammatory disorders. A biological evaluation revealed that the replacement of one methylene at the lipid tail with ether oxygen affected the inhibitory activity of 4-epi-jaspine B, leading to the identification of a selective SphK2 inhibitor.
Macrocyclic Compounds from Ansamycin Antibiotic Class as Inhibitors of PD1–PDL1 Protein–Protein Interaction
Released: August 01, 2018 | Volume 66 Issue 8 Pages 773-778
Sachin P. Patil, Suk-Chung Yoon, Abhay G. Aradhya, Jeremy Hofer, Madison A. Fink, Erika S. Enley, James E. Fisher, Marie C. Herb, Anthony Klingos, James T. Proulx, Megan T. Fedorky
STRUCTURES OF TWO NEW BITTER PRINCIPLES ISOLATED FROM A THAI MEDICINAL PLANT, VERNONIA EXTENSA D. C.
Released: March 31, 2008 | Volume 40 Issue 2 Pages 553-555
Dhavadee PONGLUX, Sumphan WONGSERIPIPATANA, Norio AIMI, Naoko OYA, Hajime HOSOKAWA, Joju HAGINIWA, Shin-ichiro SAKAI
1H-and 13C-Nuclear Magnetic Resonance Spectra of Rifampicin and 3-[(Dimethylhydrazono) methyl] rifamycin SV
Released: February 08, 2011 | Volume 36 Issue 10 Pages 4157-4161
MASAHIRO TAGUCHI, YUKINOBU YAMANE, NORIO AIKAWA, GORO TSUKAMOTO