- Mechanochemical Magnesium-Mediated Minisci C-H Alkylation of Pyrimidines with Alkyl Bromides and Chlorides
-
A novel method to synthesize 4-alkylpyrimidines by the mechanochemical magnesium-mediated Minisci reaction of pyrimidine derivatives and alkyl halides has been reported. The reaction process operates with a broad substrate scope and excellent regioselectivity under mild conditions with no requirement of transition-metal catalysts, solvents, and inert gas protection. The practicality of this protocol has been demonstrated by the up-scale synthesis, mechanochemical product derivatization, and antimalarial drug pyrimethamine preparation.
- Wu, Chongyang,Ying, Tao,Yang, Xinjie,Su, Weike,Dushkin, Alexandr V.,Yu, Jingbo
-
supporting information
p. 6423 - 6428
(2021/08/30)
-
- Preparation and application of novel quinolizine pH fluorescence molecular probe
-
The invention discloses a novel quinolizine pH fluorescence molecular probe which has brand-new action mechanism as shown in the specification, wherein a skeleton structure is 4H-quinolizine-4-imine as shown in the compound in the formula II, C-N bond in
- -
-
Paragraph 0018; 0019
(2018/04/03)
-
- Molecular Oxygen-Mediated Minisci-Type Radical Alkylation of Heteroarenes with Boronic Acids
-
The carbon-carbon bond formation via autoxidation of organoboronic acid using 1 atm of O2 is achieved in a simple, clean, and green fashion. The approach allows a technically facile and environmentally benign access to structurally diverse heteroaromatics with medicinally privileged scaffolds. The strategy also displays its practicality and sustainability in the resynthesis of marketed drugs Crestor and pyrimethamine.
- Zhang, Lizhi,Liu, Zhong-Quan
-
supporting information
p. 6594 - 6597
(2017/12/26)
-
- Phenylpyrazolo[1,5-a]quinazolin-5(4 H)-one: A suitable scaffold for the development of noncamptothecin topoisomerase i (Top1) inhibitors
-
In search for a novel chemotype to develop topoisomerase I (Top1) inhibitors, the pyrazolo[1,5-a]quinazoline nucleus, structurally related to the indenoisoquinoline system precursor of well-known Top1 poisons, was variously decorated (i.e., a substituted
- Taliani, Sabrina,Pugliesi, Isabella,Barresi, Elisabetta,Salerno, Silvia,Marchand, Christophe,Agama, Keli,Simorini, Francesca,La Motta, Concettina,Marini, Anna Maria,Di Leva, Francesco Saverio,Marinelli, Luciana,Cosconati, Sandro,Novellino, Ettore,Pommier, Yves,Di Santo, Roberto,Da Settimo, Federico
-
supporting information
p. 7458 - 7462
(2013/10/21)
-
- HETEROCYCLIC COMPOUNDS FOR THE INHIBITION OF PASK
-
Disclosed herein are new heterocyclic compounds and compositions and their application as pharmaceuticals for the treatment of disease. Methods of inhibiting PAS Kinase (PASK) activity in a human or animal subject are also provided for the treatment of diseases such as diabetes mellitus.
- -
-
Page/Page column 50-51
(2012/11/08)
-
- Discovery and characterization of a novel 7-aminopyrazolo[1,5-a]pyrimidine analog as a potent hepatitis C virus inhibitor
-
We describe a novel 7-aminopyrazolo[1,5-a]pyrimidine (7-APP) derivative as a potent hepatitis C virus (HCV) inhibitor. A series of 7-APPs was synthesized and evaluated for inhibitory activity against HCV in different cell culture systems. The synthesis and preliminary structure-activity relationship study of 7-APP are reported.
- Hwang, Jong Yeon,Windisch, Marc Peter,Jo, Suyeon,Kim, Keumhyun,Kong, Sunju,Kim, Hyoung Cheul,Kim, Soohyun,Kim, Heeyoung,Lee, Myung Eun,Kim, Youngmi,Choi, Jihyun,Park, Dong-Sik,Park, Eunjung,Kwon, Jeongjin,Nam, Jiyoun,Ahn, Sujin,Cechetto, Jonathan,Kim, Junwon,Liuzzi, Michel,No, Zaesung,Lee, Jinhwa
-
p. 7297 - 7301
(2013/02/23)
-
- Use of Pyrazolo(1,5A)Pyrimidin-7-YL Amine Derivatives in the Treatment of Neurological Disorders
-
The invention relates to methods of using the compounds of the invention, including pyrazolo[1,5a]pyrimidin-7-yl amine compounds and salts thereof, as well as pharmaceutical compositions comprising the same, in the treatment of Eph receptor-related (e.g., neurological) injuries and disorders. The invention also relates to modulating the activity of an Eph receptor in a cell, stimulating neural regeneration, and reversing neuronal degeneration, by administering a compound of the invention to a cell or subject in an effective amount.
- -
-
Page/Page column 44
(2009/04/24)
-
- Organic compounds
-
The invention relates to the use of pyrazolo[1,5a]pyrimidin-7-yl amine compounds and salts thereof in the treatment of kinase dependent diseases and for the manufacture of pharmaceutical preparations for the treatment of said diseases, novel pyrazolo[1,5a]pyrimidin-7-yl amine compounds, and a process for the preparation of the novel pyrazolo[1,5a]pyrimidin-7-yl amine compounds.
- -
-
Page/Page column 37
(2008/06/13)
-
- PYRAZOLO[1,5-A]PYRIMIDIN-7-YL-AMINE DERIVATIVES FOR USE IN THE TREATMENT OF PROTEIN KINASE DEPENDENT DISEASES
-
The invention relates to the use of pyrazolo[1,5a]pyrimidin-7-yl amine compounds and salts thereof in the treatment of kinase dependent diseases and for the manufacture of pharmaceutical preparations for the treatment of said diseases, novel pyrazolo[1,5a]pyrimidin-7-yl amine compounds, and a process for the preparation of the novel pyrazolo[1,5a]pyrimidin-7-yl amine compounds.
- -
-
Page/Page column 78
(2008/06/13)
-
- New 2,3-substituted 4,7-dihydro-6-(1'H-pyrazol-3'-yl)pyrazolo[1,5-a]pyrimidin-7-ones and related compounds: Synthesis and benzodiazepine receptor binding study
-
The reaction between two series of 7-dimethylaminovinyl pyrazolo[1,5-a]pyrimidines 4(a-r) 7a, 7d, 7f, 7(h-j) and hydrazine in acetic acid is investigated. The structure of 4,7-dihydro-6-(1'H-pyrazol-3'-yl)pyrazolo[1,5-a]pyrimidin-7-ones 5(a-r) and 7-methyl-6-(1'H-pyrazol-3'-yl)pyrazolo[1,5a]pyrimidines 8a, 8d, 8f, 8(h-j) are attributed to the isolated products and the pathway of this reaction is suggested. The in vitro benzodiazepine receptor (BzR) affinity of the title compounds are determined by testing their ability to displace 3H-flunitrazepam from its specific binding in bovine brain membranes. The IC50 and GABA (γ-aminobutyric acid) ratio values give valuable indications about affinity and behavioural profile of these new BzR ligands. Included in this investigation are indicated several structure affinity relationships of the title compounds.
- Selleri,Bruni,Costanzo,Guerrini,Casilli,Giusti,Lucacchini,Martini
-
p. 679 - 687
(2007/10/03)
-