This study describes the synthesis of fourteen thiazinanones from a multicomponent reaction of 2-morpholinoehtylamine (as primary amine), arenealdehydes (as carbonyl compound) and the mercaptopropionic acid using both conventional (thermal heating) and ultrasound methodologies. Through thermal heating methodology, the thiazinanones were obtained in 49 to 97% yields for 16 hours and through sonochemistry methodology, the reaction time was reduced for 25 minutes with yields 41 to 88%. The full identification and characterization of unpublished heterocycles were achieved by proton (1H) and carbon 13 (13C) nuclear magnetic resonance (NMR) spectroscopy, mass spectrometry and infrared. Some of them were also characterized by elemental analysis.

The efficient synthesis of fifteen novel thiazolidin-4-ones from reaction of 3-(aminomethyl) pyridine (3-picolylamine), arenealdenhydes and mercaptoacetic acid was described. The desired compounds were obtained in moderated to good yields by two methodologies: conventional heating and ultrasound irradiation. The thiazolidin-4-ones were fully identified and characterized by nuclear magnetic resonance (NMR), gas chromatography coupled to mass spectrometry (GC‑MS) and high resolution mass spectrometry (HRMS) techniques. Four compounds showed radical scavenger activity in the 2,2’-azinobis-3-ethyl-benzothiazoline-6-sulfonic acid (ABTS) assay.

The synthesis and reactivity of α-oxoketenes dithioacetals (S,S-acetals), general structure [(R¹C=OC(R²)=C(SR³)(SR4)], are reported. We also showed the application of S,S acetals as synthons for efficient synthesis of isoxazoles, pyrazoles, indazoles, thiophenes, dithiol thiones, pyridines, pyrimidines and other heterocycles. This work aims to review the importance of α-oxoketenes dithioacetals in organic chemistry during the past few years.

The development of new antiretroviral drugs is a dynamic process that is continuously fueled by identification of new molecular targets and new compounds for know targets. The current available drugs can be classified into five categories: nucleoside analogues reverse transcriptase inhibitors, non-nucleoside reverse transcriptase inhibitors, protease inhibitors, integrase inhibitors and entry inhibitors (fusion inhibitors and CCR5 antagonist). In addition, the maturation inhibitors may be considered as potential target for chemotherapeutic intervention. This review presents some anti-HIV agents that have already gone through the advance development process for final approval for the treatment of AIDS.

Este trabalho mostra a síntese de 1,2-bis-(5'-trialometilisoxazol-3'-il)etanos (3-6) e 1,2-bis(5'-trialometilpirazol-3'-il)etanos (7-10) a partir da ciclocondensação de 1,1,1,10,10,10-hexahalo-4,7-dimetoxideca-3,7-dien-2,9-dionas (1 e 2) com hidroxilamina e hidrazinas. Também é mostrada a síntese dos 1,2-bis(5'-alcoxicarbonilpirazol-3'-il)etanos (11-14) via reação da dienona 2, triclorometil-substituída, e hidrazina.

The synthesis of 1,2-bis(5'-trihalomethylisoxazol-3'-yl)ethanes (3-6) and 1,2-bis(5'-trihalomethylpyrazol-3'-yl)ethanes (7-10) from the cyclocondensation of 1,1,1,10,10,10-hexahalo-4,7-dimethoxydeca-3,7-dien-2,9-diones (1 and 2) with hydroxylamine and hydrazines is reported. In addition, the one-pot synthesis of 1,2-bis(5'-alkoxycarbonylpyrazol-3'-yl)ethanes (11-14) by reaction of chloro-substituted dienone 2 and hydrazines is also described.