17465-94-0Relevant academic research and scientific papers
Synthesis and herbicidal evaluation of aryloxyphenoxypropiona te derivatives containing purine moiety
Shi, Jianjun,Ren, Guihua,Dai, Zhimeng,Wu, Ningjie,Weng, Jianquan,Xu, Tianming,Liu, Xinghai,Tan, Chengxia
, p. 15 - 20 (2018)
series of purinoxyphenoxypropionates were designed and synthesized by introducing 8-(trifluoromethyl)-9H-purine into the aryloxyphenoxypropionate backbone. Methods: The products were characterized by 1H NMR and HRMS. Results and Conclusion: Preliminary bioassays indicated that most of the compounds exhibited good herbicidal activity at 200 mg/L.
A One-Pot Synthesis of Highly Functionalized Purines
Zelli, Renaud,Zeinyeh, Wa?l,Haudecoeur, Romain,Alliot, Julien,Boucherle, Benjamin,Callebaut, Isabelle,Décout, Jean-Luc
supporting information, p. 6360 - 6363 (2017/12/08)
Highly substituted purines were synthesized in good to high yields through a one-pot straightforward metal-free scalable method, using the Traube synthesis adapted to Vilsmeier-type reagents. From 5-amino-4-chloropyrimidines, new 9-aryl-substituted chloropurines and intermediates for peptide nucleic acid synthesis were prepared. Variant procedures allowing a rapid synthesis of ribonucleosides and 7-benzylpurine from 5-amidino-6-aminopyrimidines are also reported to illustrate the high potential of this versatile toolbox. This route appears to be particularly interesting in the field of nucleic acids for a direct and rapid access to various new 8-alkylpurine nucleosides.
An efficient synthesis of 4,6-substituted pyrrolo[3,2-d]pyrimidines by silver-catalyzed cyclization of acetylene amine
Xie, Rui,Hu, Ying,Wan, Huixin,Hu, Yanwei,Chen, Shaohua,Zhang, Shilei,Zhang, Yinan
supporting information, p. 2418 - 2421 (2016/05/19)
A silver catalyzed cyclization of acetylene amine was developed to synthesize 4,6-substituted pyrrolo[3,2-d]pyrimidine, a bioactive isosteric scaffold of purine. Starting from simple commercially available acetylenes and pyrimidines, the method was found
COMPOUNDS FOR TREATING CYSTIC FIBROSIS
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Page/Page column 84; 99; 111, (2016/06/28)
The present invention relates to compounds of Formula (I) or pharmaceutically acceptable enantiomers, salts, solvates or prodrugs thereof. The invention further relates to the use of the compounds of Formula (I) for the treatment of cystic fibrosis. The invention also relates to a process for manufacturing compounds of Formula (I).
Enhanced selectivity for inhibition of analog-sensitive protein kinases through scaffold optimization
Zhang, Chao,Shokat, Kevan M.
, p. 5832 - 5838 (2008/02/03)
The ability to inhibit any protein kinase of interest with a small molecule is enabled by a combination of genetics and chemistry. Genetics is used to modify the active site of a single kinase to render it distinct from all naturally occurring kinases. Next, organic synthesis is used to develop a small molecule, which does not bind to wild-type kinases but is a potent inhibitor of the engineered kinase. This approach, termed chemical genetics, has been used to generate highly potent mutant kinase-specific inhibitors based on a pyrazolopyrimidine scaffold. Here, we asked if the selectivity of the resulting pyrazolopyrimidines could be improved, as they inhibit several wild-type kinases with low-micromolar IC50 values. Our approach to improve the selectivity of allele-specific inhibitors was to explore a second kinase inhibitor scaffold. A series of 6,9-disubstituted purines was designed, synthesized, and evaluated for inhibitory activity against several kinases in vitro and in vivo. Several purines proved to be potent inhibitors against the analog-sensitive kinases and exhibited greater selectivity than the existing pyrazolopyrimidines.
