454-07-9Relevant articles and documents
3-Acetamido-4-(cyclooctylamino)nitro-benzene
Gonzalez-Platas,Ruiz-Perez,Torres,Yanes
, p. 651 - 654 (1997)
The crystal and molecular structure of the title compound, N-(2-cyclooctylamino-4-nitrophenyl)acetamide, C16H23N3O3, has been determined as part of an investigation into substituted benzene derivatives having no
Development of a scalable synthesis of a vascular endothelial growth factor receptor-2 kinase inhibitor: Efficient construction of a 6-etherified [1,2,4]triazolo[1,5-a]pyridine-2-amine Core
Ishimoto, Kazuhisa,Fukuda, Naohiro,Nagata, Toshiaki,Sawai, Yasuhiro,Ikemoto, Tomomi
, p. 122 - 134 (2014/05/20)
A practical and scalable synthesis of the vascular endothelial growth factor receptor-2 (VEGFR-2) kinase inhibitor 1 has been developed. The key features of the process development include facile preparation of the key raw material 3-amino-4- fluorophenol, chemoselective nucleophilic aromatic substitution of 5-chloro-2-nitropyridine with phenol, a safe one-pot synthesis of a substituted urea using an isothiocyanate generated in situ from inexpensive materials, and improvement of the yield of acylation in the end game. The optimized six-step synthesis afforded 1·H2O in 54% overall yield, twice as much as the yield of the original synthesis, without chromatographic purification. In addition, a robust recrystallization procedure to afford the desired crystal form of 1 was also developed.
3 -CYANO- 5 -ARYLAMINO-7 -CYCLOALKYLAMINOPYRROLO [1, 5 -A] PYRIMIDINE DERIVATIVES AND THEIR USE AS ANTITUMOR AGENTS
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Paragraph 000151; 000152; 000153, (2013/10/21)
The invention relates to chemical compounds of Formula (I): or a salt thereof. In some embodiments, the invention relates to inhibitors of CK2. In still further embodiments, the invention relates to pharmaceutical compositions comprising compounds disclosed herein and their use in the prevention and treatment of CK2-related conditions and diseases, e.g., cancer.