A mild and highly efficient one-pot three-component reaction for carbon-sulfur bond formation catalyzed by potassium tert-butoxide

Potassium tert-butoxide has been found to be a highly efficient catalyst for one-pot,three-component reaction of aryl aldehydes, acetophenones,and thiols via Claisen-Schmidt/Michael addition reactions for the synthesis of thia-Michael adducts in high yields. The reactions are best carried out in tert-butyl alcohol at room temperature.

Markovnikov addition of vinyl acetate with azoles catalyzed by potassium tert-butoxide

A simple and efficient methodology for Markovnikov addition of azoles with vinyl acetate catalyzed by potassium tert-butoxide is described.N-heterocyclic compounds are synthesized from simple and commercially available starting materials under mild conditions in high yields.

The role of organic electron donors in the initiation of BHAS base-induced coupling reactions between haloarenes and arenes

Coupling reactions between haloarenes and arenes(including heteroarenes)that are conducted without added transition metals but in the presence of KOtBu or NaOtBu,have been a topic of great interest since their discovery in 2008.Diverse organic structures act as additives that assist these reactions.These additives are converted into organic electron donors by the butoxide base and this leads to initiation of the coupling reactions,which proceed by radical chain mechanisms.This review provides an overview of the initiation stages of these reactions.

Synthesis of Block Copolymers of 2-Ethylhexyl Methacrylate, n-Hexyl Methacrylate and Methyl Methacrylate via Anionic Polymerization at Ambient Temperature

It still remains a concern to break through the bottlenecks of anionic polymerization of polar monomers, such as side reactions, low conver- sion and low temperature （-78 ℃）. In this work, potassium tert-butoxide （t-BuOK） was chosen to initiate the anionic polymerization of 2-ethylhexyl methacrylate （EHMA） in tetrahydrofuran. The conversions were above 99% at 0 or 30 ℃, and above 95% at 60 ℃ without side reaction inhibitors. The high conversions implied t-BuOK could suppress the side reactions. A series of block copolymers of EHMA, n-hexyl methacrylate （HMA） and methyl methacrylate （MMA） were further synthesized at 0 ℃, and the conversions were all above 99%. The GPC and IH NMR results confirmed the successful synthesis of the block copolymers. The molecular size of monomer and the state of t-BuOK （free ion pairs or aggregates） remarkably affected the polymerization rates and the molecular structures of the products. The DMA results indicated that the glass transition temperatures of PEHMA or PHMA block and PMMA block were 20 ℃ and 60 ℃, respectively, which deviated from -2 ℃ and 105 ℃ of homopolymer, respectively, due to the partial com- patibility of the blocks. This work explored a route of the anionic polymerization of polar monomers at room temperature.

A Simple and Highly Efficient Preparation of Structurally Diverse Aryl β-diketoacids as HIV-1 Integrase Inhibitors

In order to provide a facile and practical access to structurally diverse aryl -diketoacids, An improved and highly efficient oxalylation method was developed which employed commercially available and cheap reagents. The oxalylation of aryl methyl ketones, the key step to construct the pharmacophore of aryl -diketoacids, was con-siderably facilitated by a new combination of dimethyl oxalate as an oxalic source and sodium tert-butoxide as a base. A wide variety of aryl -diketoacids bearing different functional groups can be prepared rapidly in high yields at room temperature with this method, which has significant advantages over the previously reported procedures in a wider application range, much less amount of reagents, pretty higher yields and quite shorter reaction time. The bis-aryldiketoacids 3k and 3l, readily prepared by this method, displayed interesting and promising inhibitory ac-tivities against HIV-1 integrase and HIV-1 replication in cells.