PYRANOPYRAZOLES ARE FUSED HETEROCYCLIC COMPOUNDS THAT EXHIBIT A WIDE RANGE OF BIOLOGICAL ACTIVITIES [1]. DUE TO THEIR BIOLOGICAL SIGNIFICANCE, THERE HAS BEEN CONSIDERABLE INTEREST IN DEVELOPING SYNTHETIC METHODS FOR PREPARATION OF PYRANOPYRAZOLE DERIVATIVES.FUSION OF PYRIMIDINE MOIETY WITH DIFFERENT HETEROCYCLE SCAFFOLDS GIVES RISE TO A NEW CLASS OF HYBRID HETEROCYCLES POSSESSING IMPROVED ACTIVITY [2].HEREIN WE WISH TO DESCRIBE THE SYNTHESIS OF NOVEL HYBRIDE COMPOUNDS, BASED ON A PYRANOPYRAZOLE AND A PYRIMIDINE. IN THIS WORK, FIRSTLYNOVEL 3-METHYL CARBOXYLATE SUBSTITUTED PYRANO [2,3-C] PYRAZOLES WERE PREPARED BY A CATALYST-FREE FOUR-COMPONENT REACTION OF DIMETHYL ACETYLENEDICARBOXYLATE, HYDRAZINE HYDRATE, MALONONITRILE AND AROMATIC ALDEHYDES IN WATER. THEN REACTION OF PYRANOPRRAZOLE DERIVATIVES WITH PHENYL ISOTHIOCYANATE IN PYRIDINE GAVE PYRANOPYRAZOLEPYRIMIDINE HYBRIDS (SCHEME 1).

IN RECENT YEARS, SYNTHESIS OF PYRANO-PYRIMIDINONE DERIVATIVES HAVE ATTRACTED MANY INTERESTS BECAUSE OF THE DIVERSE BIOLOGICAL PROPERTIES SUCH AS ANTI-TUMOR, CARDIOTONIC, HEPATOPROTACTIVE, ANTIBACTERIAL, ANTI-BRONCHITIC, ANTI-HYPERTENSIVE, ANTI-ALLERGICA AND ANTI-FUNGAL ACTIVITIES. DUE TO THEIR...

IODINE IS USED AS A USEFUL LEWIS ACID FOR VARIOUS ORGANIC TRANSFORMATIONS DUE TO ITS NON-TOXIC, NONMETALLIC, READY AVAILABILITY, AND ENVIRONMENTALLY BENIGN NATURE. THE SAME CATALYST HAS ALSO BEEN EXPLOITED FOR A DIVERSE RANGE OF MULTICOMPONENT REACTIONS AS WELL AS THE SYNTHESIS OF VARIOUS...

BACKGROUND: THIAZOLIDINE IS A CLASS OF COMPOUNDS WHICH MERIT SPECIAL ATTENTION BECAUSE IT BELONGS TO A GROUP OF SUBSTANCES WITH ACTIVITY IN MEDICINAL CHEMISTRY. THIS NUCLEUS IS ASSOCIATED WITH ANTIBACTERIAL, ANTIFUNGAL, ANTIVIRAL, ANTITUBERCULOSIS, ANTICANCER, AND ANTIPARASITE BIOLOGICAL ACTIVITIES [1-3]. HANTZSCH THIAZOLE SYNTHESIS IS ONE OF THE BEST AND MOST WIDELY USED ROUTES TO PRODUCE THIAZOLES AND THIAZOLIDINES [4]. THE MOST COMMON REAGENTS ARE THIOUREAS (OR THIOAMIDES) AND A-HALO KETONES. AS PART OF OUR CURRENT STUDIES ON THE DEVELOPMENT OF NEW ROUTES IN APPROACH TO THE SYNTHESIS OF HETEROCYCLIC COMPOUNDS2, WE DESCRIBE AN EFFICIENT SYNTHESIS OF DIHYDROTHIAZOLOPYRIMIDINE DERIVATIVES IN IONIC LIQUID AS A GREEN SOLVENT...

RECEPTOR TYROSINE KINASES SUCH AS VEGFR2 (VASCULAR ENDOTHELIAL GROWTH FACTOR RECEPTOR 2, KDR) OR EGFR (EPIDERMAL GROWTH FACTOR RECEPTOR) PLAY CRUCIAL ROLES IN A VARIETY OF DISEASES, SUCH AS CANCER [12]. RECENTLY, SOME PYRROLOPYRIMIDINES WERE SHOWN TO BE POTENT EGFR INHIBITORS [3]. ...

BACKGROUND: BREAST CANCER, A COMPLEX AND INTRINSICALLY HETEROGENEOUS DISEASE, PRESENT A SERIOUS CLINICAL PROBLEM AND POSE SIGNIFICANT SOCIAL AND ECONOMIC IMPACTS ON THE HEALTHCARE SYSTEM. DESPITE GREAT ADVANCES IN UNDERSTANDING THE MOLECULAR ETIOLOGY OF CANCER, THERAPEUTIC STRATEGIES AGAINST THESE DISEASES ARE STILL LARGELY LACKING. THEREFORE, ACCELERATION OF THE DISCOVERY OF NEW THERAPEUTIC AGENTS FOR THIS DISEASE IS OF ENORMOUS INTEREST...

THE IMPORTANCE OF FUSED PYRIMIDINES, AS COMMON SOURCES FOR NEW POTENTIAL THERAPEUTIC AGENT, IS WELL KNOWN. BICYCLIC AND TRICYCLIC COMPOUNDS CONTAINING PYRIMIDINE SYSTEM ARE COMMON BIOLOGICALLY ACTIVE STRUCTURES. PYRIMIDINE DERIVATIVES EXHIBIT A RANGE OF PHARMACOLOGICAL ACTIVITIES SUCH AS ANTIBACTERIAL, ANTICANCER AND ANTIINFLAMMATORY [1, 2]. ...