An alternative approach toward the simple and robust synthesis of highly substituted peptidic thiazole derivatives using Ugi-multicomponent reaction (U-MCR) is described. Thus, we introduced the enantiopure (R)-2-methyl-2-isocyano-3-(tritylthio)propanoate as a novel class of isocyanide in MCR. This bifunctional isocyanide was found to undergo mild cyclodehydration to afford thiazole containing ...

A convenient zinc(II) chloride-catalyzed regioselective propargylation/amination/cycloisomerization process has been developed for the synthesis of substituted pyrrole derivatives from propargylic acetates, enoxysilanes and primary amines. Various aromatic and aliphatic propargylic acetates participate well in the reaction, providing the propargylation/amination/cycloisomerization products in g...

It is now known that multicomponent protein assemblies strictly regulate many protein functions. The S100 protein family is known to play various physiological roles, which are associated with alternative complex formations. To prepare sufficient amounts of heterodimeric S100A8 and S100A9 proteins, we developed a method for bicistronic coexpression from a single-vector system using Escherichia ...

A new multicomponent domino reaction for rapid and regioselective synthesis of highly functionalized benzo[h]pyrazolo[3,4-b]quinolines has been established. The reaction can be conducted by using readily available and inexpensive substrates under microwave irradiation within short periods of 10-26 min. Good to excellent chemical yields (61-91%) and complete regioselectivity have been achieved f...

Conventional ‘one by one’ synthesis approach has been a major rate limiting step in the systematic exploration of increasingly complex materials for the demanding new technologies. New concepts of ‘combinatorial chemistry’ are presented for the substantially efficient and cost-effective parallel synthesis and optimization of variety of multicomponent compounds as well as artificially designed l...

Al-MCM-41 nanoreactors is found to be a remarkable efficient catalyst for one-pot multicomponent cyclocondensation of benzil, aniline or ammonium acetate and aromatic aldehydes for the synthesis of polysubstituted imidazoles under solvent-free conditions. The reaction was efficiently promoted by 10 mg nano-Al-MCM-41 and the heterogeneous catalyst was recycled for four runs in this reaction with...

In this study, silica nanoparticles were used as support to prepare a new heterogeneous catalyst system for application in organic reactions. The reaction of silica nanoparticles with sodium 2-bromoethane-1-sulfonate resulted in the connection of a sulfonic acid group on the surface of silica nanoparticles (NSESA). The synthetic catalyst system was characterized using different microscopic and ...

The morpholine and piperazine with their remarkable physical and biochemical properties are popular heterocycles in organic and medicinal chemistry used in rational property design. However, in the majority of cases these rings are added to an existing molecule in a building block approach thus limiting their substitution pattern and diversity. Here we introduce a versatile de novo synthesis of...

explores the design space by considering alternate implementations during high level synthesis. Also, thermal prooling of rtl designs is too time consuming and is not viable for large designs. For almost all the examples, MSS produces better results and executes much faster than the hierarchical rtl partitioning. For smaller designs, scheduling overhead can be reduced through approximate estima...