31255-57-9Relevant 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; 0049-0051, (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.
Synthetic method for loratadine intermediate
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Paragraph 0030; 0031, (2017/08/28)
The invention specifically relates to a synthetic method for a loratadine intermediate, belonging to the technical field of chemistry. The loratadine intermediate has a structure formula as described in the specification. The synthetic route of the synthetic method is as defined in the specification. The synthetic method is characterized by comprising the following steps: adding a compound 2 in a reaction solvent 1, then adding NCS (N-chlorosuccimide) or NBS (N-bromosuccimide) and an initiator in a reflux state and carrying out a reaction so as to obtain a compound 3; adding the compound 3 into a reaction solvent 2, then adding magnesium powder and iodine and carrying out a reaction under the protection of nitrogen so as to obtain a compound 4; and adding the compound 4 into a reaction solvent 3 and reacting the compound 4 with a compound 5 under palladium-carbon catalysis so as to synthesize a target product 1. The synthetic method provided by the invention avoids usage of hazardous reagents like n-butyllithium and does not need protection of a cyano group at first and then deprotection; and the compound 1 is a key loratadine intermediate, and simplification of synthesis of the intermediate is of important significance to synthesis of loratadine.