107285-30-3Relevant articles and documents
Preparation method of loratadine intermediate 3-[2-(3-chlorphenyl) ethyl]-2-pyridinecarbonitrile
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, (2022/01/20)
The invention provides a preparation method as shown in a formula I and a preparation method of 3-[2-(3-chlorphenyl) ethyl]-2-pyridinecarbonitrile. The invention provides a novel method for preparing a loratadine intermediate.
Preparation method of loratadine intermediate
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, (2021/04/29)
The invention provides a preparation method of a loratadine intermediate, and belongs to the technical field of chemical medicine preparation. The preparation method comprises the following steps: by taking trimethyl-2-cyanopyridine as an initial synthesis raw material, protecting cyano by tert-butyl alcohol to obtain an intermediate 2, performing nucleophilic substitution on the intermediate 2 and benzyl chloride to obtain an intermediate 3, performing deprotection by using phosphorus oxychloride to obtain an intermediate 4, and finally performing addition with a Grignard reagent and obtaining a key intermediate 1 of loratadine under an acidic condition.
Aza-analogue dibenzepinone scaffolds as p38 mitogen-activated protein kinase inhibitors:Design, synthesis, and biological data of inhibitors with improved physicochemical properties
Karcher, Solveigh C.,Laufer, Stefan A.
supporting information; experimental part, p. 1778 - 1782 (2010/03/01)
We recently described a promising novel class of p38 mitogen activated protein (MAP) kinase inhibitors with dibenzepinone-scaffolds. To optimize their physicochemical properties, characterized by calculated log P values and measured lipophilicity (chromatographic hydrophobicity index=CHI), we synthesized aza-analogue dibenzepinones. Here, we present the synthesis and biological data of compounds with the novel aza-dibenzepinone scaffolds. Although these aza-analogues revealed an improved aqueous solubility, introduction of nitrogen was not effective in the p38 MAPK enzyme assay.