271242-70-7Relevant articles and documents
Novel quinazoline derivative LU1506, preparation method and applications thereof
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Paragraph 0034; 0035, (2016/11/14)
The invention discloses a novel quinazoline derivative LU1506 and a preparation method thereof. The derivative is chemically named as N-{[(4-dimethylamino)phenyl]methyl}-4-N-[7-methoxyl-6-(2-pyrrolidyl)hydroxyethyl]quinazoline-4-yl}benzene-1,4-diamine. The provided quinazoline derivative, pharmaceutically acceptable salts, solvates, and hydrates thereof have an excellent in-vitro/in-vivo antitumor activity on MCF-7, SK-BR-3, MDA-MB-468, U-118 MG, HTC116, and U-87 MG, and can be used to prepare antitumor drugs.
Polymethylhydrosiloxane (PMHS)/trifluoroacetic acid (TFA): a novel system for reductive amination reactions
Patel, Jay P.,Li, An-Hu,Dong, Hanqing,Korlipara, Vijaya L.,Mulvihill, Mark J.
scheme or table, p. 5975 - 5977 (2010/01/18)
Polymethylhydrosiloxane (PMHS)/trifluoroacetic acid (TFA) was discovered as a novel metal-free system for reductive amination reactions. A variety of (het)aryl amines as well as a representative carbamate and urea were successfully alkylated by benzaldehyde in the presence of PMHS and TFA in dichloromethane at room temperature in moderate to excellent yields (28-87%). Furthermore, this reaction protocol was successfully applied to the alkylation of p-nitroaniline with a wide range of aldehydes, ketones, and a representative acetal to obtain the alkylated products in yields ranging from 40% to 92%. The current work represents one of the very few examples of PMHS being activated by a Br?nsted acid.