A novel and efficient synthesis of 4-phenyl-2-chloropyrimidines from acetophenone cyanoimines
A versatile and efficient 2 step synthesis of 4-phenyl-2-chloropyrimidines is described. The reaction proceeds by treatment of acetophenone cyanoimines under Vilsmeier-Haack conditions to give the target compounds in moderate yields.
Cuccia, Salvatore J.,Fleming, Linda B.,France, Donald J.,Wood, William W.
ACRYLANILIDE DERIVATIVE, PREPARATION METHOD THEREFOR, AND APPLICATIONS THEREOF IN PHARMACY
Disclosed in the present invention are an acrylanilide compound represented by general formula (I) and a pharmaceutically acceptable salt thereof. The acrylanilide compound and the pharmaceutically acceptable salt thereof are used for treating clinical diseases by mainly acting on EGFR family casein kinases.
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Paragraph 0061; 0062
(2018/11/21)
DERIVATIVES OF MACROCYCLIC N-ARYL-2-AMINO-4-ARYL-PYRIMIDINE POLYETHERS AS INHIBITORS OF FTL3 AND JAK
The present invention relates to a compound with the following formula: formula (I) or a salt and/or a pharmaceutically acceptable solvate thereof, in particular for use as a drug, in particular in the treatment of cancer, as well as to the pharmaceutical compositions that contain same and to the methods for preparing same.
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Paragraph 0523-0526
(2017/10/26)
Synthesis and evaluation of the NSCLC anti-cancer activity and physical properties of 4-aryl-N-phenylpyrimidin-2-amines
Reported herein are efforts to profile 4-aryl-N-phenylpyrimidin-2-amines in terms of their anti-cancer activity towards non small-cell lung carcinoma (NSCLC) cells. We have synthesized new 4-aryl-N-phenylpyrimidin-2-amines and assessed them in terms of their cytotoxicity (A549, NCI-H187, MCF7, Vero & KB) and physicochemical properties (logD7.4 and solubility). 13f and 13c demonstrated potent anti-cancer activity in A549 cells (0.2 μM), compared to 0.4 μM for the NSCLC drug Doxorubicin. 13f also displayed low experimental logD7.4 (2.9) and the best solubility (~40 μM). Compounds 13b and 13d showed the best balance of A549 anti-cancer activity and selectivity. 13g showed good activity and selectivity comparable with the anti-cancer drug Doxorubicin.
Toviwek, Borvornwat,Suphakun, Praphasri,Choowongkomon, Kiattawee,Hannongbua, Supa,Gleeson, M. Paul
supporting information
p. 4749 - 4754
(2017/09/29)
Synthesis of 4-substituted 2-(4-methylpiperazino)pyrimidines and quinazoline analogs as serotonin 5-HT2A receptor ligands
(Chemical Equation Presented) The addition reaction of lithium reagents to the 4 position of 2-chloropyrimidine or 2-chloroquinazoline followed by oxidation of the resultant dihydro intermediate product is a powerful tool for the synthesis of 4-substitute