57614-92-3Relevant articles and documents
PIPERIDINE DERIVATIVES FOR USE IN THE TREATMENT OF PANCREATIC CANCER
-
Page/Page column 21; 60, (2018/03/01)
The present invention relates to novel piperidine derivatives having better cell growth inhibitory activities toward cancer cell cultures and, more particularly, PANC-1 cancer cell cultures than FK866. Accordingly, the present invention relates to compoun
Platinum-Catalyzed, Terminal-Selective C(sp3)-H Oxidation of Aliphatic Amines
Lee, Melissa,Sanford, Melanie S.
supporting information, p. 12796 - 12799 (2015/10/28)
This Communication describes the terminal-selective, Pt-catalyzed C(sp3)-H oxidation of aliphatic amines without the requirement for directing groups. CuCl2 is employed as a stoichiometric oxidant, and the reactions proceed in high yield at Pt loadings as low as 1 mol%. These transformations are conducted in the presence of sulfuric acid, which reacts with the amine substrates in situ to form ammonium salts. We propose that protonation of the amine serves at least three important roles: (i) it renders the substrates soluble in the aqueous reaction medium; (ii) it limits binding of the amine nitrogen to Pt or Cu; and (iii) it electronically deactivates the C-H bonds proximal to the nitrogen center. We demonstrate that this strategy is effective for the terminal-selective C(sp3)-H oxidation of a variety of primary, secondary, and tertiary amines.
Synthesis of a C-iminoribofuranoside analog of the nicotinamide phosphoribosyltransferase (NAMPT) inhibitor FK866
Gillig, Annabelle,Majjigapu, Somi Reddy,Sordat, Bernard,Vogel, Pierre
experimental part, p. 34 - 42 (2012/03/07)
FK866 (also named APO866 or WK175) is a potent NAMPT inhibitor being evaluated (Phase II) as a potential anticancer drug. The preparation of the C-iminoribofuranoside analog (2E)-N-[4-(1-benzoylpiperidin-4-yl)butyl]-3-{3- [(2S,3S,4R,5R)-3,4-dihydroxy-5-(h