| abstract |
The present invention provides a method for industrially advantageous production of 1,4-benzoxazine compounds useful as pharmaceuticals while avoiding safety and health risks. Specifically, the present invention comprises three steps shown in the following scheme, ie, a step of converting the 7-position amino group of compound [a] to a dimethylylamino group, a step of coupling compound [b] and a boronic acid compound, and Provided is a method for producing a 1,4-benzoxazine compound [A], which comprises a step of converting the 7-position of the compound [c] into a monomesylamino group. [In the above scheme, Ms represents a methanesulfonyl group, R ′ and R ″ represent a hydrogen atom, etc.] |