10425-64-6Relevant academic research and scientific papers
Synthesis of the NK3 receptor antagonist AZD2624 in C-14-, H-3- and C-13-labeled forms
Elmore, Charles S.,Dorff, Peter N.,Powell, Mark E.,Hall, James E.,Simpson, Thomas R.
experimental part, p. 239 - 246 (2012/01/15)
In support of a program to develop an antipsychotic treatment for schizophrenia, three labeled forms of the NK3 receptor antagonist AZD2624 have been prepared. [3H2]AZD2624 was synthesized by tritiodehalogenation for use in receptor
Synthesis of [14C] - and [13C6]-labeled tipranavir and its potential hydroxyl metabolite and the glucuronide conjugate
Latli, Bachir,Hrapchak, Matt,Easter, John A.,Stolle, Wayne T.,Grozinger, Karl,Krishnamurthy, Dhileepkumar,Senanayake, Chris H.
experimental part, p. 314 - 320 (2009/04/11)
Tipranavir or Aptivus is a non-peptidic protease inhibitor approved for the combination treatment with ritonavir of HIV infection. Tipranavir labeled with radioactive and stable isotopes of carbon was required for drug metabolism (excretion, distribution,
Synthesis of the carbon-14 labeled isotopomers of (R)-N-methyl-3-[2- methylphenoxyl]-benzenepropanamine hydrochloride (atomoxetine hydrochloride, LY139603), and two of its metabolites
Kuo, Fengjiun,Clodfelter, Dean K.,Wheeler, William J.
, p. 615 - 625 (2007/10/03)
Carbon-14 labeled Straterra (Atomoxetine HC1, LY139603, (-)-N-methyl-3-(2-methylphenoxy)-benzenepropanamine hydrochloride), a potent inhibitor of the presynaptic norepinephrine transporter, and two of its major metabolites were synthesized. The key compon
Heterocyclization Reaction of α-Imino Carbonyl Compounds - Derivatives of 2,5-Dihydro-1H-imidazole Nitroxides
Roshchupkina, Galina A.,Pervukhina, Natalie V.,Rybalova, Tatjana V.,Gatilov, Yuri V.,Burdukov, Alexey B.,Reznikov, Vladimir A.
, p. 4432 - 4437 (2007/10/03)
α-Imino carbonyl compounds - derivatives of 3-imidazoline nitroxides - were found to undergo heterocyclization reactions, yielding oxazole and 1,3,5-triazine derivatives. The most probable course of the reaction was suggested by the radioactive label meth
Synthesis of [carbonyl-14C]-4-benzoylbenzoic acid, a photolabelling reagent
Gomis, Jean-Marie,Santolini,Andre,Noel
, p. 1175 - 1182 (2007/10/03)
[carbonyl-14C]-4-Benzoylbenzoic acid, a photolabelling reagent, was synthesised with high specific activity in 57% radioactive yield from [carboxyl-14C]-benzoic acid. Radioactive synthesis allowed elucidation of the mechanism of a previous unlabelled synthesis using benzoic acid, methyl ester. An improvement in the experimental conditions led to a new synthesis of radioactive benzoylbenzoic derivatives with good yield.
Distinction between polar and electron-transfer routes. A mechanistic study on the wittig reactions of nonstabilized ylides
Yamataka, Hiroshi,Nagareda, Katsushi,Takatsuka, Tsutomu,Ando, Katsuhiro,Hanafusa, Terukiyo,Nagase, Shigeru
, p. 8570 - 8576 (2007/10/02)
The Wittig reaction of nonstabilized ylides with benzaldehyde and benzophenone was investigated in detail by means of carbonyl-14C kinetic isotope effects, substituent effects, and isotope-scrambling and probe experiments. The reaction with benzophenone gave the carbon isotope effects and the Hammett ρ values of considerable magnitude both in Li salt-free and salt-present conditions. In contrast, they are quite small for the reaction with benzaldehyde. Enone-isomerization and dehalogenation probe experiments indicated that the nonstabilized ylide has enough ability to transfer an electron to benzaldehyde and benzophenone. These results were interpreted in a self-consistent manner by the mechanism that the Wittig reaction of nonstabilized ylides proceeds via initial electron transfer from the ylide to the carbonyl compounds. The electron-transfer step is rate-determining for benzaldehyde, while radical coupling following the electron-transfer step is rate determining for benzophenone. From the probe experiments together with the isotope effects and the substituent effects reported previously, the reaction of semistabilized ylides was concluded to proceed through a polar nucleophilic addition mechanism.
Studies on the metabolism of propafenone. 1st comm.: Synthesis and chromatographic/mass spectrometric properties of the labelled compound and of the reference substances
Hege,Weymann,Lietz
, p. 843 - 849 (2007/10/02)
The synthesis of 14C-propafenone and 2H-propafenone (propafenone: 2-(2'-hydroxy-3'-propylamino-propoxy)-ω-phenyl-propiophenone hydrochloride) and some reference compounds is described. The thin-layer chromatographic, high-performance liquid and gas chromatographic properties of the substances are described. Propafenone and the reference substances were studied by mass spectrometry and compared with each other, with respect to structural elucidation of the metabolites. The chromatographic and mass spectrometric data (key ions) enables the metabolites of propafenone to be identified in biological material.
