Method of Synthesizing 6,7-Substituted 4-Anilino Quinazoline
申请人:Shih Kae-Shyang
公开号:US20100267949A1
公开(公告)日:2010-10-21
A method of synthesizing 6,7-substituted 4-anilino quinazoline employs 3,4-substituted benzoic acid as an initial reactant, and the 6,7-substituted 4-anilino quinazoline is obtained by an esterifying step, a nitrating step, a reducing step, a cyclizing step, and an one-pot reaction. In the above method, the initial reactant has low cost and yield. of the 6,7-substituted 4-anilino quinazoline is high, therefore, production cost can be reduced effectively, and competitive power of the product of the 6,7-substituted 4-anilino quinazoline can be improved.
A process for producing a quinazolin-4-one compound having the formula:
[wherein R
1
, R
2
, R
3
and R
4
each represents a group not participating in the below-mentioned reaction, and R
1
, R
2
, R
3
and R
4
can be combined together to form a ring] which comprises reacting an anthranilic acid derivative having the formula:
[wherein R
5
is a hydrogen atom or a hydrocarbyl group] with a formic acid derivative in the presence of an ammonium carboxylate.