1,4-benzoxazine compounds are an important class of heterocyclic compounds. Ever since 1,4-benzoxazine was discovered in 1959, it has attracted chemists due to its unique physiological activities, and their synthesis and application have been studied. However, the traditional synthesis methods of 1,4-benzoxazines have some drawbacks, such as complicated steps, harsh reaction conditions and low yield. Therefore, it is still a significant direction to develop new and efficient synthesis methods. In this paper, the synthesis methods and reaction mechanisms of these compounds are reviewed, and the application prospect of 1,4- benzoxazine and its derivatives as a dominant active structure in the future is discussed.