Teaching of Organic Chemistry of Cultivating Applied Pharmaceutical Talents

In order to effectively cultivate applied pharmaceutical talents,aiming at the current teaching situation of organic chemistry,the basic course of pharmaceutical specialty,including the problems of curriculum setting,experimental teaching,and the integration of classroom and professional knowledge,it is proposed to overcome the problem of curriculum setting by combining"online+offline"in teaching.It should overcome the problems in experimental teaching with the help of virtual simulation platform.By cultivating students organic chemistry thinking and paying attention to the integration of subject and professional knowledge,students recognition of organic chemistry course can be improved,and the quality of training can be improved.

Bimolecular reduction of carbon dioxide: double synthons for alkynes trifunctionalization

Carbon dioxide reduction, as a sustainable and versatile strategy for the access of chemical fuels, has attracted increasing attention and enormous efforts have been devoted to it in recent years. However, employing carbon dioxide as double synthons via bimolecular reduction remains challenging. Here, by leveraging the bimolecular reduction of carbon dioxide to carbonyl and methyl respectively, we describe a Pd-catalyzed trifunctionalization of alkynes with aryl iodide for the first time and showcase its advantages on the formation of various β-diketones and their application in the constructing of heterocyclic compounds with important biological activity, including pyrimidine, oxazole, pyrazole.

Palladium-Catalyzed anti-Markovnikov Halosulfonamidation of Unactivated Alkene

Palladium-catalyzed regioselective amination of unactivated alkene remains a challenge and is of great interest.Herein,a three-component coupling of unactivated alkene,sulfonamide,and N-halo compounds accessing vicinal haloamine has been conceived.This aminohalogenation represents a modular and regioselective strategy.The electrophilic halogenating agent enables regioselective anti-Markovnikov aminopalladation and facilitates subsequent halogenation events.And this protocol is characterized by gram-scale syntheses and late-stage functionalizations.Of note,the recovered byproduct phthalimide allows for reusing by conversion to the starting material.

Palladium-Catalyzed Sequential Cyclization/Functionalization of Oxime Ethers with Unactivated Vinyl Ethers for Tunable Assembly of Structurally Diverse Isoxazoles

A novel and viable palladium-catalyzed sequential cyclization/functionalization of alkynone O-methyloximes with unactivated vinyl ethers under aerobic conditions was described.The structure of the products could be successfully controlled by varying the nature of the substituents of the vinyl ethers.This new approach provides a convenient and straightforward synthetic protocol for the preparation of structurally diverse 4-(1-alkoxyvinyl)-isoxazoles and 4-vinylisoxazoles in moderate to good yields with highly regioselectivity.Remarkably,this protocol can be performed on a gram scale,showing the promising application in synthetic and pharmaceutical chemistry.