Method for preparing 2-aldehyde oxazole

Abstract

The invention relates to a method for preparing 2-aldehyde oxazole, comprising the steps of selecting commercial material on the market or easily-prepared oxazole as original raw material; dropping n-butyllithium to the organic phase solution of the main material oxazole at low temperature; and adding N-formoxyl piperidine to the reaction system, and obtaining solid lithium salt with high nuclear magnetic purity. The nuclear magnetic purity is higher than 98.0% stably and the yield is 75.0-85.0%. The synthetic method for obtaining 2-aldehyde oxazole by diluted acid hydrolysis has stable process condition, moderate chemical reaction conditions, simple operation and low pollution during the whole production and provides a new idea and a method for preparing 2-aldehyde oxazole.

Description

(1) Technical field: The invention relates to a method for preparing oxazole compounds, in particular to a method for preparing 2-formyl oxazole. (two) background technology: Oxazole is a five-membered ring containing O and N atoms in the 1 and 3 positions. It is a liquid with a pyridine-like odor and is easily soluble in water. It is a very stable compound. It is very stable in hot strong acids and does not undergo self-oxidation. reaction and does not participate in any normal biochemical process. Oxazole compounds are a class of important heterocyclic compounds. Some compounds with oxazole rings have biological activity, and they are also widely used in intermediates and drug synthesis. Oxazole-2-carboxaldehyde is to increase an aldehyde group substitution on the oxazole ring, which increases the reactivity of oxazole, and can be synthesized by a conventional biochemical process to have a biologically active compound with an oxazole ring. In intermediates, It has a wide...

AI Technical Summary

Problems solved by technology

At this stage, the method for preparing 2-formyl oxazole is mainly the organolithium reagent method. First, the lithiation reaction of oxazole and organolithium occurs, and then reacts with N,N-dimethylformamide or N-formylmorpholine On the aldehyde group, the post-treatment of these two methods is relatively cumbersome. The method of using N,N-dimethylformamide on the aldehyde group needs to obtain the product through silica gel column chromatography. Because the product has a low boiling point and high water solubility The characteristics of this method lead to a very low yield. This method is not suitable for large-scale production. The product obtained is an oily mixture by using the method of N-formylmorpholine reaction on the aldehyde group. The pure product compound of the product cannot be obtained, and it is not suitable for storage and transport