- Preparation method of medicine for treating breast cancers
-
The invention provides a preparation method of a medicine for treating breast cancers, in particular to a novel method for preparing N-{3-chloro-4-[(3-fluorobenzyl)methoxyl]phenyl}-6-[5-({[2-(methylsulfonyl)ethyl]amino}methyl)furan-2-yl]-4-quinazoline ami
- -
-
-
- Lapatinib a novel process for the preparation of
-
The present invention provides a preparation method of lapatinib. The method comprises contacting a compound shown as a formula 1 with a compound shown as a formula 2 to produce a compound shown as a formula 3; reducing the compound shown as the formula 3 to produce a compound shown as a formula 4; contacting a compound shown as a formula 5 with N,N-dimethylformamide dimethyl acetal to produce a compound shown as a formula 6; contacting the compound shown as the formula 6 with the compound shown as the formula 4 to produce a compound shown as a formula 7; in the presence of an acid, an alkali and NaNH(OAc)3, contacting a compound shown as a formula 8 with a compound shown as a formula 9 to produce a compound shown as a formula 10; in the presence of a catalyst and an alkali, contacting the compound shown as the formula 10 with a compound shown as a formula 11 to produce a transition intermediate, and contacting the transition intermediate with the compound shown as the formula 7 and p-toluenesulfonic acid to produce a compound shown as a formula I; through use of the method, the lapatinib can be effectively prepared.
- -
-
-
- Synthesis of Lapatinib via direct regioselective arylation of furfural
-
A new synthesis of Lapatinib, an orally active drug for breast cancer, is described. The synthesis involves a palladium catalyzed regioselective arylation of furfural with 6-bromo-N-(3-chloro-4-((3-fluorobenzyl)oxy)phenyl)quinazolin-4-amine. This key step replaces an atom inefficient Suzuki cross coupling reaction used in a previously disclosed route and significantly shortens the synthesis.
- Erickson, Greg,Guo, Jiasheng,McClure, Mike,Mitchell, Mark,Salaun, Marie-Catherine,Whitehead, Andrew
-
p. 6007 - 6010
(2015/01/08)
-
- QUINAZOLINE DERIVATIVES,PREPARATION METHODS AND USES THEREOF
-
The present invention has disclosed a compound of formula I and a pharmaceutically acceptable salt or a solvate thereof, wherein the substituents are as defined in the description. The invention has also disclosed a method for preparing the compound of formula I, the pharmaceutical compositions comprising the same and their uses in the preparation of an anti- tumor medicament.
- -
-
Page/Page column 16
(2008/12/08)
-
- Quinazoline Derivatives, Preparation Methods and Uses Thereof
-
The present invention has disclosed a compound of formula I and a pharmaceutically acceptable salt or a solvate thereof, wherein the substituents are as defined in the description. The invention has also disclosed a method for preparing the compound of formula I, the pharmaceutical compositions comprising the same and their uses in the preparation of an anti-tumor medicament.
- -
-
Page/Page column 9
(2009/01/20)
-