PREPARATION METHODE OF QUINAZOLINE DERIVATIVES OR AN INTERMEDIATE OF THE SAME

Various embodiments of the present invention are related to an improved method of manufacturing various types of quinazoline derivatives or intermediates thereof, which can manufacture quinazoline derivatives or intermediates thereof with high yield and purity while being industrially economical and easy to manufacture compared to an existing manufacturing method. In addition, according to various embodiments, an improved method of manufacturing one of the quinazoline derivatives, such as gefitinib, 4-(3′-chloro-4′-fluoroanilino)-7-methoxy-6-(3-morpholinopropoxy) quinazoline can be provided, which can manufacture gefitinib with high yield and purity while being industrially economical and easy to manufacture compared to an existing manufacturing method. The present invention provides the method for manufacturing quinazoline derivatives or intermediates thereof comprising steps of: conducting a reaction of a compound represented by chemical formula 1 in a solvent by putting an acid catalyst; and conducting a reaction of the compound represented by chemical formula 1 and a compound represented by chemical formula 2, thereby manufacturing a compound represented by chemical formula 3. 본 발명의 다양한 실시예에서는, 다양한 종류의 퀴나졸린 유도체 또는 이의 중간체의 개선된 제조방법에 관한 것으로, 종래의 제조방법에 비해 산업적으로 경제적이고, 제조가 용이하면서도 높은 수율 및 순도로 퀴나졸린 유도체 또는 이의 중간체를 제조할 수 있다. 또한 본 발명의 다양한 실시예에서는, 퀴나졸린 유도체의 한 종류인 제피티닙, 4-(3'-클로로-4'-플루오로아닐리노)-7-메톡시-6-(3-모르폴리노프로폭시)퀴나졸린의 개선된 제조방법을 제공할 수 있다. 종래의 제조방법에 비해 산업적으로 경제적이고, 제조가 용이하면서도 높은 수율 및 순도로 제피티닙을 제조할 수 있다.