Cyclooctyne and cycloocten-5-yne undergo, at room temperature, a 1,3-dipolar cycloaddition with dialkyl acetylenedicarboxylates 1a,b to generate furan-derived short-lived intermediates 2, which can be trapped by two additional equivalents of 1a,b or alternatively by methanol, phenol, water or aldehydes to yield polycyclic products 3b-d, orthoesters 4a-c, ketones 5 or epoxides 6a,b, respectively...

An efficient and experimentally rapid protocol for the synthesis of hitherto unreported 2,3-dicarboalkoxy-4-aroyl/heteroaroyl/alkanoyl thiophenes has been developed via 1-2 (C-S) and 3-4 (C-C) bond connections promoted by 4-dimethylaminopyridine (DMAP). Optimally, the reaction takes only 3-5 min when β-oxodithioester and dialkyl acetylenedicarboxylate are stirred in DCM at room temperature in t...

Derivatives of thiazolidinone ring systems are known to act as anti-HIV infections , analgesic, anti-bacterial, anti-convulsant, anti parasitic, potential anti-inflammatory and herbicidal agents. Due biological activities of thiazolidinones ring, several methods for their synthesis have been illustrated in literature. Imidazolidine-2-thiones were synthesized by the oxidative cyclization of 1-be...

We present herein the synthesis in good yields of two series of highly functionalized thiazolidinone derivatives from the reactions of various 4-phenyl-3-thio-semicarbazones with ethyl 2-bromoacetate and diethyl acetylenedicarboxylate, respectively.

derivatives of thiazolidinone ring systems are known to act as anti-hiv infections , analgesic, anti-bacterial, anti-convulsant, anti parasitic, potential anti-inflammatory and herbicidal agents. due biological activities of thiazolidinones ring, several methods for their synthesis have been illustrated in literature. imidazolidine-2-thiones were synthesized by the oxidative cyclization of 1-be...

The reaction of dimethyl acetylenedicarboxylate with OH-acid such as 2-naphthol in the presence of trimethyl or triphenyl phosphite under solvent-free conditions produce oxaphosphaphenanthrene derivatives in good yields. Also, the reaction of dimethyl acetylenedicarboxylate and trimethyl phosphite in the presence of 1-naphthol leads to succinate derivatives in excellent yields. Using triethyl p...

A convenient synthesis of different types of polyfunctional dihydropyrrol-2-ones via one-pot four component reactions of formaldehyde, dialkyl acetylenedicarboxylates and amines, catalyzed by trichloroacetic acid (Cl3CCO2H) at room temperature has been investigated. The significant advantages of this synthetic method are mild reaction conditions, available and inexpensive material, short reacti...