A kinetic study of product cleavage reactions from the solid phase by a biocompatible and removable cleaving reagent, HCl [0.03%]
一种生物相容的、可移去的裂解试剂HCl从固相裂解反应产物的动力学研究
Bing Yan,Ranran Shi,Bin Zhang et al.
Bing Yan et al.
TFA has been widely used as a cleaving reagent in solid-phase organic synthesis. However, it is difficult to remove from the final product, and it is toxic to various cells. To search for an alternative, we studied the kinetics of HCl cleav...
Synthesis of flavonoid analogues as scaffolds for natural product-based combinatorial libraries [0.03%]
作为基于天然产物组合文库支架的黄酮类似物合成
Nianhuan Yao,Aiming Song,Xiaobing Wang et al.
Nianhuan Yao et al.
The design and synthesis of flavonoid analogues as combinatorial scaffolds is reported. Using commercially available materials, we synthesized chalcones with fluoro and carboxy groups. Nitration of these compounds generated highly functiona...
AgOTf-catalyzed three-component reactions of 2-alkynylbenzaldehydes, amines, and diethylphosphite. An efficient route to 2,3-disubstituted-1,2-dihydroisoquinolin-1-ylphosphonates [0.03%]
由2-炔基苯甲醛、胺和二乙基磷酰胺在AgOTf催化下合成的三组分反应高效合成2,3-位取代的1,2-二氢异喹啉-1-基磷酸盐的新方法
Wei Sun,Qiuping Ding,Xiaoyu Sun et al.
Wei Sun et al.
AgOTf was discovered as a highly efficient catalyst in reactions of 2-alkynylbenzaldehydes, amines, and diethylphosphite, which provided a facile and efficient pathway for the synthesis of 2,3-disubstituted-1,2-dihydroisoquinolin-1-ylphosph...
Ultra-easy access to NH2-functionalized TSILs, their potential as highly volume-efficient electrophile scavengers, and insights into the electronics of Girard's reagent T, a venerable chemical work horse [0.03%]
超易得的NH2功能化TSILs、其作为高效体积型亲电子试剂清除剂的应用前景及古老化学工作马Girard试剂T的电子性质之洞见
Morgan D Soutullo,Carl I Odom,E Alan Salter et al.
Morgan D Soutullo et al.
2beta-(N-substituted piperazino)-5alpha-androstane-3alpha,17beta-diols: parallel solid-phase synthesis and antiproliferative activity on human leukemia HL-60 cells [0.03%]
2β-（取代的哌嗪-N）-5α-雄甾烷-3α,17β-二醇：并行固相合成及其对HL-60白血病细胞增殖的影响
Jenny Roy,Patrick DeRoy,Donald Poirier
Jenny Roy
Leukemia is the most common cancer affecting children. A steroid possessing a methylpiperazine nucleus was recently reported to inhibit the proliferation of HL-60 leukemia cells. To speed up the development of this promising potential new d...
Pyrazolo[1,5-a]pyrimidines. Identification of the privileged structure and combinatorial synthesis of 3-(hetero)arylpyrazolo[1,5-a]pyrimidine-6-carboxamides [0.03%]
吡唑并嘧啶的结构优化及杂芳基取代吡唑并嘧啶羧酸酰胺类化合物的组合合成及其活性研究
Brian T Gregg,Dmytro O Tymoshenko,Dana A Razzano et al.
Brian T Gregg et al.
The pyrazolo[1,5-a]pyrimidine class of compounds has been identified as a privileged structure for library synthesis on the basis of several key characteristics of the core molecule. A chemical set in excess of 400 compounds was synthesized...
Ting-Shan Chan,Chia-Chen Kang,Ru-Shi Liu et al.
Ting-Shan Chan et al.
The present investigation aims at the synthesis of (Y2-xEuxBiy)O3 red phosphor materials using the combinatorial chemistry method. We developed square-type arrays consisting of 90 compositions to obtain the optimum composition of co-dopants...
Synthesis of solution-phase phosphoramidite and phosphite ligand libraries and their in situ screening in the rhodium-catalyzed asymmetric addition of arylboronic acids [0.03%]
溶液相磷酰胺和膦ite配体库的合成及其在铑催化不对称加成反应中芳香硼酸的原位筛选
Richard B C Jagt,Patrick Y Toullec,Ebe P Schudde et al.
Richard B C Jagt et al.
Herein, we report the automated parallel synthesis of solution-phase libraries of phosphoramidite ligands for the development of enantioselective catalysts. The ligand libraries are screened in situ in the asymmetric rhodium-catalyzed addit...
Application of a novel design paradigm to generate general nonpeptide combinatorial templates mimicking beta-turns: synthesis of ligands for melanocortin receptors [0.03%]
一种新型设计范例的应用：生成模仿β-转角的非肽组合模板并合成促黑激素受体配体
Thomas R Webb,Luyong Jiang,Sergey Sviridov et al.
Thomas R Webb et al.
We report the further application of a novel approach to template and ligand design by the synthesis of agonists of the melanocortin receptor. This design method uses the conserved structural data from the three-dimensional conformations of...
Dianqing Sun,Richard E Lee
Dianqing Sun
A thymidinyl dipeptide urea library with structural similarity to the nucleoside peptide class of antibiotics was designed and synthesized. To generate the library, a solid-phase synthesis was developed starting from 5'-azidothymidine attac...