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Mild and high-yielding synthesis is described for raloxifene via piperdine nucleophilic substitution of a new raloxifene intermediate 3-aroyl-2-aryl-substituted benzo[b]thiophenes, which is obtained by acylation of para-substituted benzoyl chlorides and 2-arylbenzo[b]thiophenes. The key step is solvent free and offers valuable advantages, such as low cost, and is suitable for industrial production. 相似文献
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JunBoWANG ChunHaoYANG XueMingYAN XiHartWU YuYuanXIE 《中国化学快报》2005,16(7):859-862
The novel bone-targeted agents were designed and synthesized by the combination of raloxifene and bisphosphonates. The anti-osteoporosis effect was evaluated by bone mineral density (BMD) obtained from OVX mice in vivo. The results indicated that the compound 8, 9 not only prevented ovariectomy induced loss of bone but also enhanced BMD to 0.87% and 19.67% compared to Sham, respectively. 相似文献
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We report a rapid and reliable HPLC-UV method for determination of raloxifene, a kind of selective estrogen receptor modulator (SERM), in rat tissue. Proteins were precipitated by adding 200 microL of acetonitrile and 50 microL of methanol to 100 microL of the tissue homogenates, following vortex mixing and centrifugation. Separation was carried out on a reversed-phase C(18) column (150 x 4.6 mm, 5 microm) with a mobile phase of acetonitrile:0.05 m ammonium acetate (pH 4.0 +/- 0.1; 33:67, v/v) at a flow rate of 1.0 mL/min. The UV detection wavelength was set at 289 nm and the temperature of column was kept at 23 degrees C, without interference from endogenous tissue compounds. The calibration curve was linear from 0.0125 to 10.0 microg/mL with correlation coefficient of over 0.994, while the limit of quantification was 0.008 microg/mL. The intra- and inter-day coefficients of variation were less than 10% (RSD). The recovery of assay was between 95.8 and 104.5%. Furthermore, the method was used to measure the concentration of raloxifene in rat tissue after a simple oral dose. The highest level was observed in liver, lung, spleen, then heart and kidney. The lowest level was found in brain. These results suggest that raloxifene distributes rapidly and moderately into tissues such as liver, lung and spleen. 相似文献
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Tijana Raki Biljana Jan
i‐Stojanovi Andjelija Malenovi Darko Ivanovi Mirjana Medenica 《Journal of Chemometrics》2012,26(10):518-525
This paper presents a newly developed demasking large dummy effects (DDE) approach for identification of significant factor interactions in Plackett–Burman experimental design. Dummy factors, as imaginary factors, are not expected to contribute to the model, so the appearance of their high effect values could indicate the significance of the interactions they are confounded with. DDE approach consists of the screening of the large estimable effects, the calculation of the interactions that contribute the most to the large dummy effects from the alias matrix, and a single pass of all subsets regressions including preselected interactions and main factors for the final model tuning. Tested on experimentally obtained data from a robustness analysis of a method for the determination of raloxifene and its four impurities, DDE approach showed to create the models that have greater statistical power than the ones described with the main factors only, which makes them more reliable and accurate for the application. Additionally, because of the interactions selection criterion and final tuning phase of the strategy, DDE approach allows the creation of models that are likely to better describe the real systems, which increases the practical value. Copyright © 2012 John Wiley & Sons, Ltd. 相似文献
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Resonance Rayleigh Scattering Method for the Determination of Raloxifene with Evans Blue 总被引:1,自引:0,他引:1
IntroductionInrecentyears ,resonanceRayleighscattering(RRS)methodasanewanalyticaltechniquehasbeenextensivelystudiedandwidelyusedtothedeterminationofsomebiologicalmacromolecules ,suchasnucleicacid ,1 4 protein5 8andheparin ,9aswellasinorganicion ,10 14 duetoitssi… 相似文献
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