PROCESS FOR THE PREPARATION OF 1-SUBSTITUTED QUINAZOLINES

WIPO Patent Application WO/2002/026719

A1

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.

JP2007511612	Quinazolinone compounds with reduced bioaccumulation
JPS6323873	BENZHYDRYLOXYETHYLPIPERAZINE DERIVATIVE, MANUFACTURE AND DRUG COMPOSITION
WO/1991/015209	SUBSTITUTED PYRIMIDINES, PYRIMIDINONES AND PYRIDOPYRIMIDINES

KAWAZOE KENTARO (JP)
TAKEFUJI NOBUO (JP)
NISHIWAKI MASANORI (JP)
TSUBOI HIROYUKI (JP)
UEMATSU RYOICHI (JP)

PCT/JP2001/008076

April 04, 2002

September 17, 2001

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FUJISAWA PHARMACEUTICAL CO (JP)
KAWAZOE KENTARO (JP)
TAKEFUJI NOBUO (JP)
NISHIWAKI MASANORI (JP)
TSUBOI HIROYUKI (JP)
UEMATSU RYOICHI (JP)

C07D239/96; (IPC1-7): C07D239/96

WO1998041514A1

1998-09-24

Nogawa, Shintaro (1-3 Nishitenma 5-chom, Kita-ku Osaka-shi Osaka, JP)

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