| 摘要 |
A process for the preparation of 1-substituted quinazolines (I) or salts thereof via a reaction of a silylated derivative of a quinazoline (II) with a chloroalkane (III) or a salt thereof in the presence of a catalytic amount of the corresponding bromoalkane (IV) or a salt thereof, wherein the reaction is conducted in two steps by conducting the reaction either with low-boiling substances formed being once removed in the course of the reaction or while removing such substances, and then adding a catalytic amount of the bromoalkane (IV) or a salt thereof to the reaction mixture, and the resulting product is desilylated. According to this process, the reaction can be completed in a short time and 1-substituted quinazolines (I) can be stably prepared from inexpensive chloroalkanes used as main raw material in high yield and at high efficiency. |
