The invention relates to a preparation method of azelnidipine, which comprises the following steps: carrying out Knoevenagel reaction on cyanoacetic acid and m-nitrobenzaldehyde used as starting materials to generate a compound 1; hydrolyzing cyano group of the compound 1 to generate a compound 2; carrying out esterification on the compound 2 and 1-diphenylmethyl-3-azetidin-ol under the action of DCC (N,N'-dicyclohexylcarbodiimide) to generate a compound 3; carrying out Hantzsch cyclization on the compound 3 and isopropyl 3-aminocrotonate under alkaline conditions to generate an azelnidipine crude product; and refining the crude product to obtain the azelnidipine fine product. The method is simple to operate and suitable for industrial production; and the reaction product is easy to separate.
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Paragraph 0013
(2017/03/08)
CO2 absorbing cost-effective ionic liquid for synthesis of commercially important alpha cyanoacrylic acids: A safe process for activation of cyanoacetic acid
Cost-effective and carbon dioxide absorbing ionic liquid, tri-(2-hydroxyethyl) ammonium acetate, was shown to perform multiple roles in Knoevenagel condensation. It acted as an environmentally benign solvent, as an activating catalyst for the less reactive cyanoacetic acid and also as a risk reduction medium for the unevenly generated large amount of CO2 gas for large scale reactions. The reaction was scaled up for multi-gram synthesis of commercially important alpha cyanoacrylic acids.
Sharma, Yogesh O.,Degani, Mariam S.
experimental part
p. 526 - 530
(2010/04/23)
Search for Potential Herbicides. Synthesis of Nitrophenyl-2-cyanoacrylamides
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Bhatia, M. S.,Sharma, Sunita,Jindal, Ritu
p. 162 - 163
(2007/10/02)
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