1219799-22-0Relevant articles and documents
DEHYDRATION OF ALCOHOLS ON ALUMINA-12
KNOEZINGER H,SCHEGLILA A
, p. 252 - 263 (1970)
Primary kinetic isotope effects of the dehydration from the gas phase of tertiary, secondary and iso-butanol on alumina have been easured between 120 and 230 C. The deuteration on the hydroxyl group does not give rise to an isotope effect, whereas substitution of the !-proton by deuterium produces an appreciable effect. Below 200 C primary, secondary, and tertiary alcohols are dehydrated via reaction intermediates over alumina which presumably contain a certain degree of ionic contributions. With increasing temperature these ionic contributions are favored.
Synthesis and evaluation of 13C-labeled 5-5-dimethyl-1-pyrroline-N-oxide aimed at in vivo detection of reactive oxygen species using hyperpolarized 13C-MRI
Saito, Keita,Sail, Deepak,Yamamoto, Kazutoshi,Matsumoto, Shingo,Blackman, Burchelle,Kishimoto, Shun,Brender, Jeffrey R.,Swenson, Rolf E.,Mitchell, James B.,Krishna, Murali C.
, p. 18 - 26 (2018/12/04)
Effective means to identify the role of reactive oxygen species (ROS) mediating several diseases including cancer, ischemic heart disease, stroke, Alzheimer's and other inflammatory conditions in in vivo models would be useful. The cyclic nitrone 5,5-Dimethyl-1-pyrroline-N-oxide (DMPO) is a spin trap frequently used to detect free radicals in vitro using Electron Paramagnetic Resonance (EPR) spectroscopy. In this study, we synthesized 13C-labeled DMPO for hyperpolarization by dynamic nuclear polarization, in which 13C NMR signal increases more than 10,000-fold. This allows in vivo 13C MRI to investigate the feasibility of in vivo ROS detection by the 13C-MRI. DMPO was 13C-labeled at C5 position, and deuterated to prolong the T1 relaxation time. The overall yield achieved for 5–13C-DMPO-d9 was 15%. Hyperpolarized 5–13C-DMPO-d9 provided a single peak at 76 ppm in the 13C-spectrum, and the T1 was 60 s in phosphate buffer making it optimal for in vivo 13C MRI. The buffered solution of hyperpolarized 5–13C-DMPO-d9 was injected into a mouse placed in a 3 T scanner, and 13C-spectra were acquired every 1 s. In vivo studies showed the signal of 5–13C-DMPO-d9 was detected in the mouse, and the T1 decay of 13C signal of hyperpolarized 5–13C-DMPO-d9 was 29 s. 13C-chemical shift imaging revealed that 5–13C-DMPO-d9 was distributed throughout the body in a minute after the intravenous injection. A strong signal of 5–13C-DMPO-d9 was detected in heart/lung and kidney, whereas the signal in liver was small compared to other organs. The results indicate hyperpolarized 5–13C-DMPO-d9 provided sufficient 13C signal to be detected in the mouse in several organs, and can be used to detect ROS in vivo.
Diarylpyrazole compound, composition containing the same and application thereof
-
Paragraph 0189; 0190; 0191, (2019/10/04)
The invention provides a diarylpyrazole compound, a composition containing the same and application thereof. The diarylpyrazole compound is the compound shown as formula (I) or its tautomer, stereisomer, prodrug, crystal form, pharmaceutically acceptable
DEUTERIUM-SUBSTITUTED OXADIAZOLES
-
Paragraph 00181, (2016/10/31)
Described are deuterated modulators of S1P1 receptors, pharmaceutical compositions thereof, and methods of use thereof.
