＜正＞The transition metal catalyzed reactions of diazo compounds have been well-established as powerful approach...
Lei Zhou,Fei Ye,Yan Zhang and Jianbo Wang~* Beijing National Laboratory for Molecular Sciences(BNLMS),Key Laboratory of Bioorganic Chemistry and Molecular Engineering of Ministry of Education,College of Chemistry,Peking University,Beijing 100871,China
A Pd（II） catalyzed tandem reaction of o-alkynylbenzaldehydes or o-alkynylbenzaldimines with substituted indoles initiated by the intermolecular addition of indoles to the carbonyl or imine group followed by the nucleopalladation of an intramolecular alkyne and quenching the carbon-palladium bond by protonolysis to regenerate the Pd（II） species was developed. The reaction can be carried out under mild conditions without the necessity of a redox system.
In the past decade, the asymmetric Morita-Baylis-Hillman (MBH)/aza-Morita-Baylis-Hillman (aza-MBH) reaction has attracted great attention because it leads to the formation of densely functionalized products in a catalytic and atom-economic way. The MBH/aza-MBH adducts can be further applied in a wide variety of organic synthesis, such as peptide synthesis and heterocyclic compounds synthesis. After a lot of attempts to improve the enantioselectivity, many types of chiral organocatalysts have been identified as highly enantioselective organocatalysts in MBH/aza-MBH reaction. Especially, certain "privileged chiral catalysts" are highly enantioselective in MBH/aza-MBH reaction, which are designed and developed through introducing bi-/multi-functional groups on the so-called "privileged structures" such as cinchona alkaloids, BINAP/BINOL. This review summarizes the exciting advances about the design and development of chiral catalysts derived from "privileged structures" and their applications in asymmetric MBH/aza-MBH reaction.
The family Picornaviridae is one of the largest families of human viral pathogens,causing an extensive range of clinical manifestations from mild fever,common cold to serious paralytic poliomyelitis,COPD,etc.,some of which can even be life-threatening.Picornaviruses also cause zoonotic epidemics that result in dramatic social and economical losses.Although no efficient antivirus agent for prophylaxis or treatment of picornarivus infections has been officially approved yet,a large number of anti-picornavirus compounds with potent activity have been developed and investigated,through which further information about picornavirus has been revealed as well.Viral mRNA translation,viral mRNA replication and especially the viral capsid are the three main targets of these compounds having been extensively studied.The typical one is the WIN series of compounds that bind to the viral capsid and inhibit rival attachment or uncoating.Herein,a perspective on picornavirus inhibitors and a concrete evolution of WIN compounds will be presented in this paper.
＜正＞Epoxides are highly versatile intermediates in organic synthesis due to their easy access and their suscept...
Tao Wang and Junliang Zhang~* Shanghai Key Laboratory of Green Chemistry and Chemical Processes,Department of Chemistry, East China Normal University,200062
A unique transformation to realize the allylic amination from vinylic bromides was described and an unexpected C-Pd migration was observed from sp2 carbon to adjacent allylic sp3 carbon initiated from vinyl bromide. Various 3-aryl-2-bromopropenes and secondary amines were surveyed and the allyl amination products were obtained in moderate isolated yields. The primary amine was not fit for this transformation. Mechanistic studies indicate that this migration went through β-hydride elimination and reverse C=C bond insertion.
