143-36-2Relevant articles and documents
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Maynard
, p. 2108,2111 (1932)
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Corbett,Williams
, p. 3437,3442 (1964)
Synthesis and biological evaluation of deuterated sofosbuvir analogs as HCV NS5B inhibitors with enhanced pharmacokinetic properties
Ao, Wangwei,Ma, Xueqin,Lin, Youping,Wang, Xiaojing,Song, Wei,Wang, Qinglin,Zhang, Xiquan,Xu, Hongjiang,Zhang, Yinsheng
, p. 215 - 229 (2019/05/07)
A series of deuterated sofosbuvir analogs were designed and prepared with the aim of improving their pharmacokinetic properties. The devised synthetic routes allow for site-selective deuterium incorporation with high levels of isotopic purity. As expected, the deuterated analogs (37-44) are as efficacious as sofosbuvir when tested in vitro inhibition of viral replication (replicon) assays. Compared with sofosbuvir, deuterated analog 40 displays improved in vivo pharmacokinetics profiles in rats and dogs in terms of the metabolite and the prodrug. The Cmax and area under the curve (AUC) of 40 in dogs were increased by 3.4- and 2.7-fold, respectively. Due to the enhanced pharmacokinetic properties and the great synthetic advantage of an inexpensive deuterium source (D2O) for 40, it was chosen for further investigation.
Raman- and infrared-spectroscopic investigations of dilute aqueous phosphoric acid solutions
Rudolph, Wolfram W.
, p. 9642 - 9653 (2011/01/10)
Phosphoric acid in water and heavy water has been studied by Raman and infrared spectroscopy over a broad concentration range (0.00873-1.560 mol kg-1) at 23 °C. The vibrational modes of the PO4 skeleton (C3v symmetry) of H3PO4(aq) and D 3PO4(D2O) have been assigned. In addition to the P-O stretching modes a deformation mode has been detected, δPO-H(D) at 1250 and 935 cm-1, respectively. In addition to the modes of the phosphoric acid and heavy phosphoric acid a mode of the dissociation product H2PO4- and D2PO4 - has been detected at 1077 cm-1 and 1084 cm-1 respectively. H3PO4 and D3PO4 is hydrated in aqueous solution which could be verified by Raman spectroscopy following the νPO and νsP(OH)3 mode as a function of temperature. These modes show a pronounced temperature dependence inasmuch as νPO shifts to higher wavenumbers with temperature increase and νsP(OH)3 to lower wavenumbers. In the range between 300-600 cm-1 the deformation modes have been observed. In very dilute H3PO4 solutions however, the dissociation product is the dominant species. The dissociation degree, α for H3PO 4(aq) and D3PO4(D2O) as a function of dilution has been measured at 23 °C. In these dilute H3PO 4(aq) and D3PO4(D2O) solutions no spectroscopic features for a dimeric species of the formula H6P 2O8 and D6P2O8 could be detected. Quantitative Raman measurements have been carried out to follow the dissociation of H3PO4 and D3PO4 over a very broad concentration range and also as a function of temperature. From the dissociation data, the pK1 value for H3PO4 has been determined to 2.14(1) and for D3PO4 to 2.42(1) at 23 °C. In the temperature interval from 24.5 to 99.7 °C the pK 1 values for H3PO4(aq) have been determined and thermodynamic data have been derived.
Oxidation of white phosphorus by peroxides in aqueous and alcoholic solutions: mechanistic aspects and catalytic studies
Akbayeva, Dina N.,Faisova, Farida Kh.,Abdreimova, Rumia R.,Peruzzini, Maurizio
, p. 181 - 193 (2008/10/09)
The oxidation of white phosphorus by hydrogen peroxide or different organic peroxides (such as tert-butyl hydroperoxide, dibenzoylperoxide, 3-chloroperoxybenzoic acid) has been studied in both aqueous and alcoholic solutions under anaerobic conditions. De
