27916-43-4Relevant academic research and scientific papers
Preparation method of 3-(2-cyanophenyl)propionic acid and 4-cyano-1-indanone
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Paragraph 0055-0059; 0065-0069, (2021/08/07)
The invention provides a preparation method of 3-(2-cyanophenyl)propionic acid and 4-cyano-1-indanone, wherein the preparation method comprises the steps: mixing 2-cyanobenzaldehyde, Meldrum's acid, formic acid and alkali, and carrying out condensation reaction on the 2-cyanobenzaldehyde and the Meldrum's acid to prepare the 3-(2-cyanophenyl)propionic acid; making 3-(2-cyanophenyl)propionic acid contact with a chlorination reagent, carrying out acylating chlorination reaction, and thus obtaining an acylating chlorination product; and carrying out Friedel-Crafts acylation reaction on the acylating chlorination product in the presence of a catalyst to prepare the 4-cyano-1-indanone. The method can improve the preparation efficiency of 3-(2-cyanophenyl)propionic acid and 4-cyano-1-indanone, and has the advantages of short route, low cost, small pollution and the like.
Method for preparing 2, 3-dihydro-1-oxo-1H-indene-4-carbonitrile
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Paragraph 0026; 0045-0048; 0057; 0058, (2020/10/05)
The invention discloses a method for preparing 2, 3-dihydro-1-oxo-1H-indene-4-carbonitrile, comprising the following steps of: carrying out a reaction between 2-cyanobenzyl bromide and 2,2-dimethyl-1,3-dioxane-4,6-dione, carrying out condensation, hydrolysis and decarboxylation, and finally carrying out Friedel-Crafts acylation, thereby obtaining the 2, 3-dihydro-1-oxo-1H-indene-4-carbonitrile. The method is simple, free of cyanide pollution and high in yield.
Preparation method of indanone intermediate
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, (2020/01/12)
The invention provides a preparation method of an indanone intermediate, and belongs to the field of pharmaceutical chemicals. The prepration method comprises the following steps: carrying out condensation reaction, hydrolysis and decarboxylation of 2-cyanobenzyl bromide or 2-cyanobenzyl chloride and dimethyl malonate in an organic solvent to obtain 2-cyanophenylpropionic acid; and reacting the obtained 2-cyanobenzene propionic acid with aluminum trichloride and an assistant agent to obtain 4-cyano-1-indanone. According to the invention, no highly toxic cyaniding reagent is needed, and the method has the advantages of high product purity, good safety, high yield, simple operation and the like. The method provided by the invention can effectively prepare the indanone intermediate, and provides favorable conditions for further preparation of ozanimod.
A Ligand-Directed Catalytic Regioselective Hydrocarboxylation of Aryl Olefins with Pd and Formic Acid
Liu, Wei,Ren, Wenlong,Li, Jingfu,Shi, Yuan,Chang, Wenju,Shi, Yian
supporting information, p. 1748 - 1751 (2017/04/11)
An effective Pd-catalyzed hydrocarboxylation of aryl olefins with Ac2O and formic acid is described. A variety of 2- and 3-arylpropanoic acids can be regioselectively formed by the judicious choice of ligand without the use of toxic CO gas.
