The sphingolipid bases, D-erythro- and D-threo-sphingosines, are the target molecules that have been synthesized to demonstrate the efficiency of a new methodology to control both absolute and relative configurations in acyclic systems. Tubulysins are compounds of extraordinary potency, rapidly degrading the tubulin cytoskeleton, with tubulysin D being the most active tubulin-modifier known so far. Among other isonitriles, isocyanoacetate derivatives occupy an important place in the field of synthetic application and reaction diversity, which makes them strongly attractive objects for investigation. The unique multifunctional nature of isocyanoacetic acid derivatives opens up a range of exciting reactions, especially tandem/cascade processes for the synthesis of complex cyclic and macrocyclic systems. Multicomponent chemistry of isocyanoacetates is also a powerful instrument to access different classes of biochemically relevant compounds such as peptides, peptide molecules, and nitrogen heterocycles.

Isocyanoacetate derivatives: synthesis, reactivity, and application.

Protection for the Amino Group

Current methods for the synthesis of 2-substituted azoles

An efficient diastereo- and enantioselective [3+2] cycloaddition reaction of α-aryl isocyanoacetates to isatins catalyzed by a quinine-derived bifunctional amine-thiourea-bearing sulfonamide as multiple hydrogen-bonding donor catalyst has been investigated. The corresponding adducts, which bear a spirocyclic quaternary stereocenter at the C-3 position of the oxindole, were obtained in good yields (51–95%), high diastereoselectivities (up to >20:1 dr) and good to excellent enantioselectivities (up to 97% ee).

Cinchona Alkaloid‐Derived Thiourea‐Catalyzed Diastereo‐ and Enantioselective [3+2] Cycloaddition Reaction of Isocyanoacetates to Isatins: A Facile Access to Optically Active Spirooxindole Oxazolines

The present invention is related to thiazole derivatives of Formula (I) in particular for the treatment and/or prophylaxis of autoimmune disorders and/or inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, bacterial or viral infections, kidney diseases, platelet aggregation, cancer, transplantation, graft rejection or lung injuries.

Thiazole derivatives and use thereof

A one-pot preparation of dimethyl n-alkyliminodithiocarbonates

A new synthetic approach to 2-alkyl-, 2-aryl-, and 2-N-alkylaminothiazoles has been carried out. This strategy is based on the high versatility of synthons derived from 2-methylthiothiazoles

A new synthetic approximation to thiazoles with a versatile persubstitution and/or perfunctionalization

Diastereoselective synthesis of functionalized 2,4-diamino-3-hydroxyglutaric acid derivatives of potential biological interest from glycine derivatives

Diastereoselective synthesis of syn,syn- and syn,anti-2,4-diamino-3-hydroxyglutaric acid derivatives from ethyl α-acyl alaninates

On the acylation reactions of aza-allyl carbanions derived from N-[bis(methylthio)methylene]glycine ethyl ester and N-[bis(methylthio)methylene]benzylamine

E. Martinez‐Santos

Papers

A one-pot preparation of dimethyl n-alkyliminodithiocarbonates

A new synthetic approximation to thiazoles with a versatile persubstitution and/or perfunctionalization

Diastereoselective synthesis of functionalized 2,4-diamino-3-hydroxyglutaric acid derivatives of potential biological interest from glycine derivatives

Diastereoselective synthesis of syn,syn- and syn,anti-2,4-diamino-3-hydroxyglutaric acid derivatives from ethyl α-acyl alaninates

On the acylation reactions of aza-allyl carbanions derived from N-[bis(methylthio)methylene]glycine ethyl ester and N-[bis(methylthio)methylene]benzylamine