An efficient one-pot synthesis of novel β-amino acid derivatives containing a thiadiazole moiety was developed using a chiral squaramide cinchona alkaloid as organocatalyst. The reactions afforded chiral β-amino acid derivatives in moderate yields and with moderate to excellent enantioselectivities. The present study demonstrated for the first time the use of a Mannich reaction catalyzed by a ch...

An efficient and original synthesis of various 2,4-disubstituted pyrido[3,2-d]pyrimidines is reported. One-pot di(het)arylation and diamination approaches were used to obtain highly functionalized products in very good yields. The two one-pot processes were compared to their step-by-step related synthesis. Both routes started from 2,4-dichloropyrido[3,2-d]pyrimidine and included a chlorine disc...

Chemical transformations are normally conducted in batch or flow mode, thereby allowing the chemistry to be temporally or spatially controlled, but these approaches are not normally combined dynamically. However, the investigation of the underlying chemistry masked by the self-assembly processes that often occur in one-pot reactions and exploitation of the potential of complex chemical systems ...

A highly efficient method for the enantioselective one-pot synthesis of 1,3-oxazolidines and 1,3-oxazinanes has been reported. The reaction proceeds via the formation of hemiaminal intermediates obtained by the enantioselective addition of respective alcohols to imines catalyzed by a chiral magnesium phosphate catalyst, followed by intramolecular cyclization under mildly basic conditions. A wid...

An N-Bromosuccinimide (NBS) promoted one pot strategy for the synthesis of α-amino functionalized aryl ketones starting from commercially available styrenes has been developed. NBS participates in multiple tasks, such as bromonium ion formation, oxidation of bromohydrin and providing a nucleophilic nitrogen source. The reaction can easily be switched between α-imido and α-amino ketones by the c...

Unripe grape juice (verjuice) as a natural catalyst was successfully applied to perform the one-pot reaction of aryl aldehydes, malononitrile, hydrazine hydrate and ethyl acetoacetate to synthesize pyranopyrazole derivatives in aqueous ethanol at room temperature in excellent yields. Furthermore, unripe grape juice catalyzed one-pot synthesis of hexahydroquinoline-3-carboxamide derivatives by t...

Step-economical syntheses of annulated 1,2,3-triazoles were accomplished through copper-catalyzed intramolecular direct arylations in sustainable one-pot reactions. Thus, catalyzed cascade reactions involving [3 + 2]-azide-alkyne cycloadditions (CuAAC) and C-H bond functionalizations provided direct access to fully substituted 1,2,3-triazoles with excellent chemo- and regioselectivities. Likewi...