A method for synthesizing 1,4-dihydropyridine derivatives

Abstract

The invention relates to a method for synthesizing 1,4-dihydropyridines derivatives. According to the method, a fluorescence-marked nonmetal organic boron-nitrogen lewis acid-alkali dual-functional complex is used as a catalyst, so that the pollution of heavy metals is effectively avoided; the catalyst can be recycled, and a residual amount of the catalyst in a product can be rapidly detected; and the source of raw materials is wide, the target yield is close to 100 percent, the reaction process is a homogenous reaction, and a product is obtained by virtue of chromatographic separation. The whole reaction system can be directly amplified, and the industrialization prospect is significant.

Description

【Technical field】 [0001] The invention belongs to the field of catalytic organic synthesis, in particular to a method for synthesizing key intermediates of lercanidipine and derivatives thereof. 【Background technique】 [0002] Organic Lewis acid-base bifunctional catalysts have been widely used in organic synthesis due to their high regio- and stereoselectivity due to their synergistic activation of nucleophiles and electrophiles. Although there are many advantages, there are also some shortcomings that cannot be ignored: it is difficult to separate, recover and reuse products and catalysts, especially in homogeneous reactions; it is difficult to quickly detect the residual amount of catalysts in products, especially in medicinal chemistry. In order to overcome the above difficulties, we designed and synthesized a class of fluorescently labeled organic boron nitrogen Lewis acid-base bifunctional catalysts (reported in the patent application number 201710133198.4), which are ...

AI Technical Summary

Problems solved by technology

Although there are many advantages, there are also some shortcomings that cannot be ignored: it is difficult to separate, recycle and reuse the product and catalyst, especially in homogeneous reactions; it is difficult to quickly detect the residual amount of catalyst in the product, especially for medicinal chemistry.

[0008] The traditional method of synthesizing 1,4-dihydropyridine is a "one-pot" synthesis using the Hantzsch reaction, which has disadvantages such as long time, complicated operation, and low yield.

After that, many researchers proposed some synthetic methods to improve the Hantzsch reaction, but there are still some defects, such as the use of expensive metal catalysts, difficult separation, low yield and rapid detection of catalyst residues in the product, etc.

Images