128924-10-7Relevant academic research and scientific papers
PHENAZINES AS INHIBITORS OF DISCOIDIN DOMAIN RECEPTORS 2 (DDR2)
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Page/Page column 27, (2020/10/21)
The invention concerns a compound of Formula (I) or a pharmaceutically acceptable salt or derivative thereof, wherein R1 and R2 are independently H or a group -O(CHR5)nR6, where n is an integer value from 1 to 3, R5 is independently H or CH3 for each integer value of n, R6 is H, an optionally substituted saturated heterocyclic ring or NR7R8, where R7 and R8 are independently H or (C1-C3)alkyl, R4 is H or CH3, R3 is a group selected from the group consisting of an optionally substituted aryl, (C3-C6)alkyl, benzyl, an optionally substituted saturated (C3-C6)cycloalkyl and an optionally substituted unsaturated heterocyclic ring for use as a medicament. The compounds as medicament are used in the treatment (DDR2)-mediated diseases and disorders such as a cancer, acute and chronic pain, osteoarthritis, inflammation-associated disorder as arthritis, rheumatoid arthritis, atherosclerosis, various fibrotic disorders, fibrosis or kidney injury.
Preparing method of Avitinib
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Paragraph 0046; 0047, (2019/11/14)
The invention discloses a preparing method of Avitinib. The method includes the following steps of A, dissolving 2,4-dichloropyrimidine, XPhos, Pd2(dba)3 and 3-floro-4-(4-methyl piperazine-1-yl)aniline in a propyl alcohol solvent for reaction to obtain an intermediate I; B, dissolving tBu-protected 3-nitrophenol in an ethyl alcohol solvent, and adding iron powder and ammonium chloride to obtain tBu-protected 3-amino-phenol; C, dissolving the tBu-protected 3-amino-phenol and diisopropylethylamine in dichloromethane, and dropwise adding isopentyl chloride for reaction to obtain an intermediate II; D, making the intermediate II flow backwards in a rifluoroacetic acid solvent, and removing tBu protection to obtain an intermediate III; E, mixing the intermediate I, the intermediate III and dimethylformamide for reaction to obtain the end product. The method is simple in operation and high in yield.
Nucleophilic Substitution of Nitrite in Nitrobenzenes, Nitrobiphenyls and Nitronaphthalenes
Effenberger, Franz,Koch, Markus,Streicher, Willi
, p. 163 - 173 (2007/10/02)
Aromatic compounds, accessible only by multistep procedures, can be synthesized easily by nucleophilic substitution of nitrite in nitrobenzenes, nitrobiphenyls, and nitronaphthalines.Thus, meta-substituted phenols 3, 4, and 7 are obtained from 1,3-dinitrobenzene (1) and meta-substituted nitrobenzenes 6, as well as 3,5-disubstituted phenols 10 and 5-substituted resorcinol derivatives 11 from 3,5-disubstituted nitrobenzenes 9.The unsymmetrically substituted nitrobiphenyls 13, 15, 17, 19, 23, 24, and 26 are also available by nitrite exchange from the corresponding easily accessible dinitrobiphenyls 16, 18, 20, 22, and 25.A nitrite exchange with nucleophiles is easily possible in the 1,5-disubstituted naphthalenes 29, 34, while in the case of the 1,8-disubstituted naphthalenes 31, 36 only the chloro derivative 36 undergoes this exchange under much stronger conditions in low yield.
