87867-14-9Relevant academic research and scientific papers
Deuterated ticagrelor derivative, preparation method and application of deuterated ticagrelor derivative in preparation of anticoagulation drugs
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Paragraph 0042; 0043; 0044, (2017/10/13)
The invention discloses a deuterated ticagrelor derivative which comprises a compound with a structure represented by a general formula (I) shown in the description and optical isomers thereof or pharmaceutically acceptable salts or solvates thereof, wher
CYCLOPROPYL MODULATORS OF P2Y12 RECEPTOR
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Page/Page column 47, (2011/02/24)
The present invention relates to new cyclopropyl modulators of P2Y12 receptor activity, pharmaceutical compositions thereof, and methods of use thereof.
HYDROXYETHYLAMINO SULFONAMIDE DERIVATIVES
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Page/Page column 86; 87; 88, (2010/11/17)
This invention relates to novel hydroxyethylamino sulfonamides, their derivatives, pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering a compound with the ability to act as an HIV (human immunodeficiency virus) protease inhibitor.
New deuterated oligo(ethylene glycol) building blocks and their use in the preparation of surface active lipids possessing labeled hydrophilic tethers
Faragher, Robert J.,Schwan, Adrian L.
, p. 1371 - 1378 (2008/04/12)
(Chemical Equation Presented) For the introduction of additional analysis protocols of tethered molecules, a method is presented to prepare functionalized, deuterated oligo(ethylene glycols) from ethylene glycol-d 4. Partial oligomerization of ethylene glycol-d4 and conversion to ditosylates is accompanied by coupling reactions to prepare doubly benzyl protected oligo(ethylene glycols) with two to five repeating units. The tetramer bearing 16 deuteria was elaborated at both ends to eventually prepare 2,3-di-O-phytanyl-sn-glycerol-1-tetraethylene glycol-D,L-α-lipoic acid ester (DPTL), which bears a fully deuterated tetra(ethylene glycol) spacer group. Through linking of functionalized components, an analogue of DPTL possessing an octa(ethylene glycol) spacer group was prepared, both in deuterated and unlabeled form.
Tandem Mass Spectrometric Approaches for the Analysis of Alkylguanines in Human Urine
Cushnir, J. R.,Naylor, S.,Lamb, J. H.,Farmer, P. B.
, p. 552 - 558 (2007/10/02)
Human exposure to carcinogenic alkylating agents can lead to the formation of covalently bound adducts in DNA, some of which are excreted in urine as alkylated purines following DNA degradation and repair.Tandem mass spectrometric methods have been developed for the qualitative and quantitative determination of such alkylpurines in human urine.Short-chain alkyl- and hydroxyalkylguanines have been synthesized with the substituents at the N-7, O6- and N2-positions of guanine.Examination of the product ion scans of their molecular ions (electron impact (EI) ionization) revealed that the ion at m/z 151, +, was common to all of the alkylguanines studied, with the exception of the methylated analogues.Precursor ion scans of this ion on partially purified human urine extracts showed the presence of several ions (e.g. m/z 179, 195) which were consistent with molecular ions for alkylguanines.The presence of these and other constituents was confirmed by product ion spectra of molecular ions (EI and fast atom bombardement), and by high-performance liquid chromatographic separation prior to tandem mass spectrometry (MS/MS).Evidence was obtained for the presence of N-7-methyl-, N2-methyl, N2-dimethyl-, N2-ethyl- and N-7-(2-hydroxyethyl)guanine.Quantitative methods were established for these five alkylguanines using gas chromatography mass spectrometry (GC/MS) and GC/MS/MS.Deuterated internal standards were synthesized and added to the urine prior to extraction of alkylpurines by Sep-Pak cartridge chromatography.The products were converted into their tert-butyldimethylsilyl derivatives and analysed by selected ion monitoring (SIM) of + or by multiple reaction monitoring (MRM) of the fragmentation M+. -> +.The MRM method yielded values for N-7-methylguanine of 2.57 +/- S.D. 1.32 mg day-1 (n=6), N2-methylguanine of 0.31 +/- 0.10 mg day-1 (n=10) and N2-dimethylguanine of 0.21 +/- 0.23 mg day-1 (n=10).N2-Ethyl- and N-7-(2-hydroxyethyl)guanine could only be detected by SIM at levels of ca. 0.5 and 2 μg day-1, respectively.The MRM analyses, although inherently less sensitive than the SIM analyses, exhibit greater selectivity and consequently fewer contaminant ions.
The Synthesis of N(τ)-(2-hydroxypropyl)histidine, N(τ)-2-hydroxyethyl)histidine, and Their Deuteriated Analogues
Campbell, John B.
, p. 1213 - 1218 (2007/10/02)
The synthesis of N(τ)-(2-hydroxypropyl)histidine (1), N(τ)-(2-hydroxypropyl)histidine (2), N(τ)-(2-hydroxyethyl)histidine (3), and N(τ)-(2-hydroxyethyl)histidine (4) by reaction of protected histidine derivatives with bromoacetone, bromoacetone, 2-benzyloxyethyl toluene-p-sulphonate (17), and 2-benzyloxyethyl toluene-p-sulphonate (18), respectively, is described.
