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
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Paragraph 0029; 0046-0048, (2021/02/10)
The invention provides a preparation method of loratadine. The method comprises the following steps: taking 2-cyano-3-methylpyridine as a raw material, and carrying out Ritter reaction, m-chlorobenzylchloride condensation, POCl3 deprotection group, Grignard reaction, cyclization and ethyl chloroformate substitution to obtain 4(8-chlorine-5, 6-dihydro-11H-benzo-[5, 6]cycloheptano[1, 2-b]pyridine-11-subunit)-1-piperidine carboxylic acid ethyl ester. According to the invention, a post-treatment process is innovated, and a new cyclization system is adopted to catalyze the reaction, so that the use of high-cost and high-toxicity strong acid is avoided, and a milder and more economical synthesis method is provided for industrial production.
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.