River discharge is the main source of terrigenous sediments in many coastal areas adjacent to estuaries and deltas of large rivers. Spreading and mixing dynamics of river plumes governs transport of suspended sediments and their deposition at sea bottom at these areas. Generally river plumes have very large synoptic and seasonal variability, which cannot be reconstructed from structure of bottom sediments due to their small accumulation velocity.
View Article and Find Full Text PDFA general and efficient asymmetric synthesis of cyclic indoline aminals was developed with a high level of 1,3-stereoinduction through a dynamic crystallization-driven condensation. Dehydrogenation of the indoline aminals with potassium permanganate produced the corresponding cyclic indole aminals in high yields and excellent enantioselectivities. This general methodology was successfully applied to the synthesis of a wide variety of chiral cyclic indoline aminals and indole aminals with aromatic and aliphatic functional groups.
View Article and Find Full Text PDFA concise, enantioselective synthesis of the HCV NS5a inhibitor MK-8742 (1) is reported. The features of the synthesis include a highly enantioselective transfer hydrogenation of an NH imine and a dynamic diastereoselective transformation. The synthesis of this complex target requires simple starting materials and nine linear steps for completion.
View Article and Find Full Text PDF[reaction: see text] A new and practical method for the synthesis of 1- and 1,3-substituted xanthines is reported. Direct base-promoted condensation of the imidazole precursor 1 with carbamates 2 gives 1-substituted 7-PMB xanthines 7 in good yields. Alkylation of these derivatives or their potassium salts proceeds under mild conditions to give functionalized 1,3-substituted 7-PMB xanthines 9 in good to excellent yields.
View Article and Find Full Text PDFCurr Opin Drug Discov Devel
November 2002
Recent methods for the synthesis of aziridines and aziridinium ions, the mechanisms of their nucleophilic ring-opening reactions and applications to the practical synthesis of pharmaceutical intermediates are reviewed.
View Article and Find Full Text PDFZh Nevropatol Psikhiatr Im S S Korsakova
November 1989
The article presents the data on 57 schizophrenic and 26 neurotic patients investigated by computerized tomography (CT). Only 4 of the neurosis patients (15.4%) displayed minor CT changes.
View Article and Find Full Text PDFAcute toxicity of ethylphosphate, diethylphosphate and metaphosphate of S-ethylisothiuronium does not differ significantly when the drugs are administered to albino female mice intraperitoneally, intramuscularly or subcutaneously. However, this toxicity diminishes 4--5-fold during intragastric administration. The substances are approximately 100 mg/kg more toxic for Wistar rats as compared to mice.
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