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Synthesis of 3?-deoxy-3?-fluorothymidine (FLT) 5?-O-glucuronide: A reference standard for imaging studies with [ 18F]FLT

Reaction of methyl 2,3,4-tri-O-acetyl-1-O-(trichloroacetimidoyl)-alpha-d- glucopyranuronate with 3?-deoxy-3?-fluorothymidine in the presence of trimethylsilyl trifluoromethanesulfonate gave (2R,3R,4S,5S,6S)-2-(((2R,3S,5R) -3-fluoro-5-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl) tetrahydrofuran-2-yl)methoxy)-6-(methoxycarbonyl)tetrahydro-2H-pyran-3,4, 5-triyl triacetate, which was hydrolysed to 3?-deoxy-3?- fluorothymidine-5?-glucuronide. Analysis of this reference standard by high performance liquid chromatography enabled the identification of [ 18F]3?-deoxy-3?-fluorothymidine-5?-glucuronide in blood samples from six human patients who had been administered [ 18F]3?-deoxy-3?-fluorothymidine.

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beta-Glucuronyl carbamate based pro-moieties designed for prodrugs in ADEPT

A number of pro-moieties 8a-e designed for prodrug preparation have been synthesized. The pro-moieties, containing a glucuronyl carbamate group linked to a spacer possessing a terminal carboxylic acid group, have been synthesized from isocyanates 6 and anomerically unprotected glucuronic acids 10. The requisite isocyanates had to be prepared using the Curtius rearrangement. Glucuronyl carbamates proved to be excellent substrates for human beta-glucuronidase. The pro-moieties 8a-e can be coupled to hydroxy- or amino group containing drugs. The resulting prodrugs are designed to be activated by beta-glucuronidase and to be used in ADEPT. Application is demonstrated with the synthesis of duanomycin prodrugs 12a-e.

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Synthetic Route of 73464-50-3, Catalysts are substances that increase the reaction rate of a chemical reaction without being consumed in the process. 73464-50-3, Name is (2R,3R,4S,5S,6S)-2-Hydroxy-6-(methoxycarbonyl)tetrahydro-2H-pyran-3,4,5-triyl triacetate, molecular formula is C13H18O10. In a Article£¬once mentioned of 73464-50-3

A general method has been developed for the formation of glycosyl chlorides and bromides from picolinic esters under mild and neutral conditions. Benchtop stable picolinic esters are activated by a copper(II) halide species to afford the corresponding products in high yields with a traceless leaving group. Rare beta glycosyl chlorides are accessible via this route through neighboring group participation. Additionally, glycosyl chlorides with labile protecting groups previously not easily accessible can be prepared.

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The discoveries of Sch 48461 and Sch 58235 and their novel pharmacology of inhibition of cholesterol absorption have prompted efforts to determine their biological mechanism of action (MOA). To this end, a series of radioiodinated analogues with good to excellent in vivo activity have been designed and synthesized as single enantiomers. They are structurally consistent with the allowable SAR of the 2-azetidinone class of cholesterol absorption inhibitors.

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Balanced chemical reaction does not necessarily reveal either the individual elementary reactions by which a reaction occurs or its rate law.Safety of (2R,3R,4S,5S,6S)-2-Hydroxy-6-(methoxycarbonyl)tetrahydro-2H-pyran-3,4,5-triyl triacetate. In my other articles, you can also check out more blogs about 73464-50-3

A catalyst don’t appear in the overall stoichiometry of the reaction it catalyzes, but it must appear in at least one of the elementary reactions in the mechanism for the catalyzed reaction. 73464-50-3, Name is (2R,3R,4S,5S,6S)-2-Hydroxy-6-(methoxycarbonyl)tetrahydro-2H-pyran-3,4,5-triyl triacetate, molecular formula is C13H18O10. In a Article£¬once mentioned of 73464-50-3, Safety of (2R,3R,4S,5S,6S)-2-Hydroxy-6-(methoxycarbonyl)tetrahydro-2H-pyran-3,4,5-triyl triacetate

Allyl (methyl 2,3,4-tri-O-acetyl-beta-D-glucopyranosyl uronate)-(1?3)-4,6-O-benzylidene-2-deoxy-2-phthalimido-beta-D- glucopyranoside (4) and benzyl (methyl 2,3,4-tri-O-acetyl-beta-D- glucopyranosyl uronate)-(1?3)-4,6-O-benzylidene-2-deoxy-2-phthalimido- beta-D-glucopyranoside (5) have been efficiently synthesized by coupling allyl 4,6-O-benzylidene-2-deoxy-2-phthalimido-beta-D-glucopyranoside (2) or benzyl 4,6-O-benzylidene-2-deoxy-2-phthalimido-beta-D-glucopyranoside (3) with methyl (2,3,4-tri-O-acetyl-1-O-trichloroacetimidoyl)-alpha-D- glucopyranuronate (1), respectively, using trimethylsilyl triflate as promoter.

Balanced chemical reaction does not necessarily reveal either the individual elementary reactions by which a reaction occurs or its rate law.Safety of (2R,3R,4S,5S,6S)-2-Hydroxy-6-(methoxycarbonyl)tetrahydro-2H-pyran-3,4,5-triyl triacetate. In my other articles, you can also check out more blogs about 73464-50-3

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A series of anthracycline prodrugs containing an immolative spacer was synthesized for application in selective chemotherapy. The prodrugs having the general structure anthracycline-spacer-beta-glycoside were designed to be activated by beta-glucuronidase or beta-galactosidase. Prodrugs with -chloro, -bromo or -n-hexyl substituents on the spacer were synthesized as well as prodrugs containing a -beta-glucuronyl, -beta-glucosyl or -beta-galactosyl carbamate specifier. The key step in the synthesis of all prodrugs is the highly beta-diastereoselective addition reaction of the anomeric hydroxyl of a glycosyl donor to a spacer isocyanate resulting in the respective beta-glycosyl carbamate pro-moieties. The resulting protected pro-moieties were coupled to an anthracycline. Prodrugs were evaluated with respect to activation rate by the appropriate enzyme and additionally, their IC50 values were determined. Optimal prodrugs in this study were at least 100- to 200-fold less toxic than their corresponding drug in vitro and were activated to the parent drug in a half-life time of approximately 2h. Copyright (C) 1999 Elsevier Science Ltd.

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The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.73464-50-3, Name is (2R,3R,4S,5S,6S)-2-Hydroxy-6-(methoxycarbonyl)tetrahydro-2H-pyran-3,4,5-triyl triacetate, molecular formula is C13H18O10. In a Patent£¬once mentioned of 73464-50-3, Quality Control of: (2R,3R,4S,5S,6S)-2-Hydroxy-6-(methoxycarbonyl)tetrahydro-2H-pyran-3,4,5-triyl triacetate

The invention is directed to the prior art by detecting the defects of the aerobic Vaginitis, discloses a sugar donor synthesis process, and then with the chromogen indole connected cheng gan, to synthesize a effect better, sensitivity, stability, specificity is relatively high indole glucoside substrate, according to the test, the present invention relates to synthetic substrate color rendering performance with the market has some aerobe group Vaginitis detection of checking the color rendering performance of the, color rendering performance superior to that […] Vaginitis detection reagent color rendering performance. The invention through the indole glycosides in the chromogenic substrate sugar donor synthesis process with connected cheng gan technological innovation, extraction and purification process innovation and application verification, which makes the product of each step the reaction yield is greatly improved, color close to white, reduces the substrate color during identification impact, greatly improves the detection sensitivity of the detecting Vaginitis aerobe group and the accuracy of the detection. (by machine translation)

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The reactant in an enzyme-catalyzed reaction is called a substrate. Enzyme inhibitors cause a decrease in the reaction rate of an enzyme-catalyzed reaction.I hope my blog about 73464-50-3 is helpful to your research., HPLC of Formula: C13H18O10

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New and greatly improved preparations of the 12alpha, 1?beta- (5) and 12beta,1?beta- (6) glucuronides of dihydroartemisinin (DHA, 2) are reported using anomeric hydroxy and imidate glucuronate intermediates. Comparison of the synthetic and natural materials shows that the human metabolite of DHA is the 12alpha-epimer 5.

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A series of nitric oxide (NO)-releasing glycosyl derivatives (2-14) of oleanolic acid were synthesized to improve the aqueous solubility and cytotoxicity of the parent compound 1. Derivative 3 exhibited better solubility and strong cytotoxicity against human hepatocellular carcinoma (HCC) in vitro. Furthermore, 3 displayed low acute toxicity to mice and significantly inhibited the growth of HCC tumors in vivo, indicating that 3 may be a promising candidate for the treatment of human HCC.

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Chemoselective microwave-assisted transesterification of 6,1-lactone derived from glucuronic acid is catalyzed by reusable Dawson-type polyoxometalates. These catalysts allow the formation of pseudo-disaccharides from easily available precursors. This permits the expeditious assembly of promising building blocks from precursors obtained from biomass, with easy recycling of the catalyst.

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