CuI催化的酰胺和溴苯的偶联反应研究

本文报道了一种新的催化体系 (CuI / 氨基酸 / K₃PO₄) 催化胺和芳香溴代化合物之间的交叉偶联反应，对于不同的底物都以较好的产率得到了产物。该反应操作简单，适用性广，并且试剂价格便宜。     

A facile synthesis of the oxazolidinone antibacterial agent linezolid

A facile synthetic route of linezolid 1 has been developed.Using commercially available(R)epichlorohydrin as the starting material,1 was obtained through a sequence of cyclization,substitution, a Goldberg coupling,aminolysis and acetylation reactions.The synthetic route is easy to perform and can be scaled up.     

Petersen Cores and the Oddness of Cubic Graphs

Let G be a bridgeless cubic graph. Consider a list of k 1‐factors of G. Let be the set of edges contained in precisely i members of the k 1‐factors. Let be the smallest over all lists of k 1‐factors of G. We study lists by three 1‐factors, and call with a ‐core of G. If G is not 3‐edge‐colorable, then . In Steffen (J Graph Theory 78 (2015), 195–206) it is shown that if , then is an upper bound for the girth of G. We show that bounds the oddness of G as well. We prove that . If , then every ‐core has a very specific structure. We call these cores Petersen cores. We show that for any given oddness there is a cyclically 4‐edge‐connected cubic graph G with . On the other hand, the difference between and can be arbitrarily big. This is true even if we additionally fix the oddness. Furthermore, for every integer , there exists a bridgeless cubic graph G such that .     

A Survey for the Spectrum of Triangles over Sequence Spaces

Abstract

In the present paper, we summarize the recent literature concerning the spectrum and fine spectrum with respect to Goldberg’s classification of some operators represented by an infinite matrix over certain sequence spaces.     

Enantioselective Aromatic Amination?

The atroposelective formation of C−N bonds has recently emerged within the field of amination reactions. On first sight, it may seem quite surprising that such an ancient class of organic coupling reactions (Gabriel, Ullmann, Goldberg, Buchwald, Hartwig and many others) has so few enantioselective solutions, and this in spite of asymmetric synthesis being now a mature concept and field. Why should enantioselective C−N bond formation be so difficult? This question and some of the first examples that promise an imminent change of paradigm are herein discussed.     

The circular chromatic index of Goldberg snarks

We determine the exact values of the circular chromatic index of the Goldberg snarks, and of a related family, the twisted Goldberg snarks.     

Synthesis of MAPA Reagents and 2-Alkyl(aryl)aminopyridines from 2-Bromopyridine Using the Goldberg Reaction

A short and economical synthesis of various 2-methylaminopyidine amides (MAPA) from 2-bromopyridine has been developed using the catalytic Goldberg reaction. The effective catalyst was formed in situ by the reaction of CuI and 1,10-phenanthroline in a 1/1 ratio with a final loading of 0.5–3 mol%. The process affords high yields and can accommodate multigram-scale reactions. A modification of this method provides a new preparation of 2-N-substituted aminopyridines from various secondary N-alkyl(aryl)formamides and 2-bromopyridine. The intermediate aminopyridine formamide is cleaved in situ through methanolysis or hydrolysis to give 2-alkyl(aryl)aminopyridines in high yields.     

Fast and selective synthesis of novel cyclic sulfamide HIV-1 protease inhibitors under controlled microwave heating

A novel and highly selective silver-promoted monobenzylation method was developed to promote synthesis of nonsymmetrical sulfamide-based HIV-1 inhibitors. Microwave-accelerated palladium-catalyzed N-amide arylation- and aminocarbonylation reactions were employed for rapid and reliable compound generation. With this class of inhibitory agents, six active inhibitors were identified, the most potent inhibitor possessing a K_i-value of 20 nM.     

Fulkersonʼs Conjecture and Loupekine snarks

Fulkersonʼs Conjecture says that every bridgeless cubic graph has six perfect matchings such that each edge belongs to exactly two of them. In 1976, F. Loupekine created a method for constructing new snarks from already known ones. We consider an infinite family of snarks built with Loupekineʼs method, and verify Fulkersonʼs Conjecture for this family.     

Amino acid-mediated Goldberg reactions between amides and aryl iodides

A highly general, experimentally simple, and inexpensive catalyst system was developed for the amidation of aryl iodides by using 5 mol % of CuI as catalyst, 20 mol % of an amino acid as ligand, and K₃PO₄ as base.