- A PROCESS FOR THE PREPARATION OF BOSUTINIB
-
The present invention provides an improved process for the preparation of bosutinib and its intermediate 2-cyano-N-(2, 4-dichloro-5-methoxyphenyl)acetamide.
- -
-
-
- Design, synthesis and pharmacokinetic evaluation of a novel series of triazole-based Src kinase inhibitors with anti-proliferative activity
-
Src has been recognized as an important therapeutic target for the treatment of cancer. A novel series of triazole-based Src inhibitors were synthesized and evaluated for their anti-proliferative activities in vitro against human lung cancer A549 cells wi
- Chen, Shaojun,Guo, Chuansheng,Shi, Shiting,Shi, Yanyan,Fang, Du,Fan, Houxing
-
scheme or table
p. 9 - 13
(2012/02/05)
-
- Synthesis and Src kinase inhibitory activity of a series of 4-[(2,4-dichloro-5-methoxyphenyl)amino]-7-furyl-3-quinolinecarbonitriles
-
Compound 1 (SKI-606, bosutinib), a 7-alkoxy-4-[(2,4-dichloro-5- methoxyphenyl)amino]-3-quinolinecarbonitrile, is a potent inhibitor of Src kinase activity. We previously reported that analogs of 1 with thiophene groups at C-7 retained the Src activity of
- Boschelli, Diane H.,Wu, Biqi,Ye, Fei,Wang, Yan,Golas, Jennifer M.,Lucas, Judy,Boschelli, Frank
-
p. 7868 - 7876
(2007/10/03)
-
- 4 [(2,4-DICHLORO-5-METHOXYPHENYL)AMINO]-6-ALKOXY-7-ETHYNYL-3-QUINOLINECARBONITRILES FOR THE TREATMENT OF ISCHEMIC INJURY
-
This invention relates to compounds of the formula (I): wherein: R is methyl or ethyl; R' and R" are independently alkyl of 1 to 3 carbon atoms, or R' and R", taken together with the nitrogen to which they are attached, can form a 5 or 6 membered saturate
- -
-
Page/Page column 13-14
(2010/11/08)
-
- Process for preparation of 4-amino-3-quinolinecarbonitriles
-
This invention discloses a process for the preparation of a 4-amino-3-quinolinecarbonitrile comprising combining an amine compound with a cyanoacetic acid and an acid catalyst to yield a cyanoacetamide; condensing the cyanoacetamide with an optionally up to tetra-substituted aniline in an alcoholic solvent and a trialkylorthoformate to yield a 3-amino-2-cyanoacrylamide; combining the 3-amino-2-cyanoacrylamide with phosphorus oxychloride in acetonitrile, butyronitrile, toluene or xylene, optionally in the presence of a catalyst to yield a 4-amino-3-quinolinecarbonitrile and also discloses a process for the preparation of a 7-amino-thieno[3,2-b]pyridine-6-carbonitrile comprising combining a disubstituted 3-amino thiophene with a cyanoacetamide and trialkylorthoformate in an alcoholic solvent to obtain a 3-amino-2-cyanoacrylamide; and combining the 3-amino-2-cyanoacrylamide with phosphorus oxychloride and acetonitrile, butyronitrile, toluene or xylene, optionally in the presence of a catalyst to yield a 7-amino-thieno[3,2-b]pyridine-6-carbonitrile and also discloses a process for the preparation of a 4-amino-3-quinolinecarbonitrile by combining an amine compound with a cyanoacetic acid and a peptide coupling reagent to obtain a suspension; filtering the suspension to yield a cyanoacetamide; condensing the cyanoacetamide with an optionally up to tetra-substituted aniline, an alcoholic solvent, and triethylorthoformate to yield a 3-amino-2-cyanoacrylamide; and combining the 3-amino-2-cyanoacrylamide with phosphorus oxychloride to yield a 4-amino-3-quinolinecarbonitrile.
- -
-
Page/Page column 6
(2010/02/10)
-
