- Microwave-assisted synthesis of phenylpyrimidine derivatives via Suzuki-Miyaura reactions in water
-
An efficient method was developed to prepare biphenylpyrimidine scaffolds via a Suzuki-Miyaura coupling reaction. In this procedure, the products were synthesized under microwave irradiation in water and analogues of biguanidine were employed as ligands.
- Le, Yi,Zhang, Yan,Wang, Qin,Rao, Nian,Li, Dan,Liu, Li,Ouyang, Guiping,Yan, Longjia
-
supporting information
(2021/02/21)
-
- Synthesis of N-pyrimidin[1,3,4]oxadiazoles and N-pyrimidin[1,3,4]-thiadiazoles from 1,3,4-oxadiazol-2-amines and 1,3,4-thiadiazol-2-amines via Pd-catalyzed heteroarylamination
-
An efficient and practical procedure was developed to prepare various N-pyrimidin[1,3,4]oxadiazole and thiadiazole scaffolds using a Buchwald-type coupling. The products of this reaction are otherwise difficult to access and could be used as building bloc
- Yan, Longjia,Deng, Minggao,Chen, Anchao,Li, Yongliang,Zhang, Wanzheng,Du, Zhi-yun,Dong, Chang-zhi,Meunier, Bernard,Chen, Huixiong
-
supporting information
p. 1359 - 1362
(2019/04/25)
-
- Pyrimidine as an Aryl C-H Activating Group
-
The Pd-catalyzed regioselective C-H activation/arylation, /iodination, and/acetoxylation reactions of 4-arylpyrimidines using aryl iodides, N-iodosuccinimide, and (diacetoxyiodo)benzene respectively as coupling partners are described. Suzuki-Miyaura coupl
- Gupta, Sahaj,Melanson, Jennifer A.,Vaillancourt, Louis,Nugent, William A.,Tanoury, Gerald J.,Schatte, Gabriele,Snieckus, Victor
-
supporting information
p. 3745 - 3748
(2018/07/22)
-
- Synthesis of 4-aryl and unsymmetrical 4,6-diarylpyrimidines by the Suzuki-Miyaura cross-coupling reaction
-
A two-step procedure for the synthesis of 4-arylpyrimidines from inexpensive 4,6-dichloropyrimidine via a Suzuki-Miyaura/hydrodechlorination reaction sequence is described. The reaction resulted in the predominant formation of mono-arylated product. The c
- Gupta, Sahaj,Melanson, Jennifer A.,Selim Hossain,Vaillancourt, Louis,Tanoury, Gerald J.,Nugent, William A.,Snieckus, Victor
-
p. 1549 - 1569
(2018/10/04)
-
- Discovery of wtRET and V804MRET Inhibitors: From Hit to Lead
-
Oncogenic activation of RET kinase has been found in several neoplastic diseases, like medullary thyroid carcinoma, multiple endocrine neoplasia, papillary thyroid carcinoma, and non-small-cell lung cancer. Currently approved RET inhibitors were not originally designed to be RET inhibitors, and their potency against RET kinase has not been optimized. Hence, novel compounds able to inhibit both wild-type RET (wtRET) and its mutants (e.g., V804MRET) are needed. Herein we present the development and the preliminary evaluation of a new sub-micromolar wtRET/V804MRET inhibitor, N-(2-fluoro-5-trifluoromethylphenyl)-N′-{4′-[(2′′-benzamido)pyridin-4′′-ylamino]phenyl}urea (69), endowed with a 4-anilinopyridine structure, starting from our previously identified 4-anilinopyrimidine hit compound. Profiling against a panel of kinases indicated 69 as a multi cKIT/wtRET/V804MRET inhibitor.
- Mologni, Luca,Dalla Via, Martina,Chilin, Adriana,Palumbo, Manlio,Marzaro, Giovanni
-
p. 1390 - 1398
(2017/09/01)
-
- PYRIMIDINE COMPOUND AND ITS USE IN PEST CONTROL
-
A pyrimidine compound represented by below formula (I) has excellent control activity against pests and is useful as an active ingredient of a pest controlling agent.
- -
-
Page/Page column 187; 188
(2010/12/18)
-
- Arylpiperazine-containing pyrimidine 4-carboxamide derivatives targeting serotonin 5-HT2A, 5-HT2C, and the serotonin transporter as a potential antidepressant
-
Pyrimidine usually has good pharmacokinetic properties as a drug substance and considerable efforts have been devoted to develop pyrimidine derivatives into drug candidates. Arylpiperazine-containing pyrimidine 4-carboxamide derivatives were synthesized and evaluated for binding to serotonin receptors and transporter. Pyrimidine derivatives showed good antidepressant activity in FST (forced swimming test) animal model and also displayed no appreciable inhibitory activity against hERG channel blocking assay. Herein SAR studies of pyrimidine derivatives targeting serotonin receptors and transporter will be disclosed.
- Kim, Jong Yup,Kim, Deukjoon,Kang, Suk Youn,Park, Woo-Kyu,Kim, Hyun Jung,Jung, Myung Eun,Son, Eun-Jung,Pae, Ae Nim,Kim, Jeongmin,Lee, Jinhwa
-
supporting information; experimental part
p. 6439 - 6442
(2010/11/18)
-
- PHARMACEUTICAL COMPOUNDS AS INHIBITORS OF CELL PROLIFERATION AND THE USE THEREOF
-
Disclosed are compounds of Formula I effective as cytotoxic agents. The compounds of this invention are useful in the treatment of a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.
- -
-
Page/Page column 12; 27-28
(2008/12/05)
-
- ANTIPROLIFERATIVE PYRIMIDYL, FUSED PYRIMIDYL AND PYRIMIDYL HYDRAZONES
-
The present invention is related to a novel series of pyrimidyl or fused pyrimidyl hydrazones. Compounds of Formula (I) wherein A is selected from the group consisting of Formulas (A1), (A2), (A3), (A4), (A5) are useful for the treatment and/or prevention of a proliferative disease.
- -
-
Page/Page column 41
(2010/11/27)
-
- Pyrimidine Synthesis - A New Method
-
A new one-step-method for the synthesis of 2-phenylpyrimidines of type I was developed by reacting benzotrichloride with various nitriles in the presence of aluminum chloride.
- Somech, Iris,Shvo, Youval
-
p. 1639 - 1641
(2007/10/03)
-
- Synthesis and reactivity of disubstituted 4,4'-bipyrimidines: Preparation of a new pentadentate ligand
-
Synthesis of 2,2'-disubstituted 6,6'-diphenyl-4,4-bipyrimidines (bpm) and their reactivity towards oxidation and bromination is investigated. Preparation of a pentadentate ligand by a template reaction from 2-bromomethyl-4,4'-bipyrimidine unit is reported
- Papet,Marsura
-
p. 478 - 481
(2007/10/02)
-