Current Organic Synthesis - Volume 15, Issue 7, 2018

Background: Among the numerous bond-forming patterns, C–C bond formation is one of the most useful tools for building molecules for the chemical industry as well as life sciences. Recently, one of the most challenging topics is the study of the direct coupling reactions via multiple C–H bond cleavage/activation processes. A number of excellent reviews on modern C–H direct functionalization have been reported by Berg Read More

Background: Spiro skeleton is an important structural motif in natural products, usually accounting for their formidable architectures and remarkable biological profiles. Recent advances demonstrated that a diverse range of scenarios held the promise for the assembly of spirocenter based on ortho-dearomatization strategy. In this article, we describe the latest development of ortho-dearomatization reaction in constr Read More

Background: Pictet-Spengler reactions is an irreplaceable part of cyclization reaction leading to the formation of indispensable heterocyclic moieties including imidazole, benzoxazole, pyrrole, indole and others having immense biological and chemical significance. Researchers have explored this reaction using different types of catalysts and reactions conditions (including solvents, acids, etc.) to ensure the better sele Read More

Background: Due to significant biological activity associated with N-, O- and S-heterocycles, a number of reports for their synthesis have appeared in recent decades. Traditional approaches require expensive or highly specialized equipment or would be of limited use to the synthetic organic chemist due to their highly inconvenient approaches. This review summarizes the applications of copper catalysts with the emphasis on Read More

Background: Benzofurans are very important structural motifs found in a great number of natural products and biologically active compounds. Many commercially available drugs, including citalopram, dronedarone, saprisartan, darifenacin, and galantamine are derived from benzofuran core entities. Due to the diversity of benzofuran derivatives in the therapeutic response profile, developing novel and truly efficient meth Read More

Aim and Objectives: Development of simple synthetic routes for widely used organic compounds from readily available reagents is one of the major tasks in organic chemistry. Therefore, new approaches for increasing the molecular diversity of simple starting materials, are needed. Herein, an efficient synthesis of imidazo[1,2-a]pyridine, pyrido[1,2-a]pyrimidine and pyrido[1,2-a][1,3]diazepine derivatives is described. Materials a Read More

Aim and Objective: During the investigation of sodium nitrite-catalyzed oxidative coupling reaction of aryls, an unprecedented C(sp2)-H and C(sp3)-H coupling of substituted 2-aryl acetonitrile was found. Materials and Methods: The structure of the coupled product was confirmed by 1H and 13C NMR spectroscopy and high-resolution mass spectrometry (HRMS), and comparison of its derivatives with known compounds. The effect Read More

Aim and Objective: To develop efficient method for the synthesis of unusual oxetanes bicycle and diversely functionalized oxetane motifs bearing medicinally relevant functional group in new chemical space and evaluation as cytotoxic agents. Materials and Methods: General procedure for the synthesis of 2, 3, 9 and 11: A mixture of L-ascorbic acid derivative 1 or 8 or 10 (10 mmol) and benzophenone (12 mmol) in dry benzene Read More

Aim and Objective: Reaction of phthalic anhydride (1) with thiocarbohydrazide (2) in methanol gave the intermediate (6) whose boiling in water or ethanol gave N-(1,3-dioxoisoindol-2-yl)aminothiocarbohydrazide (5); where its Condensation with aldehydes and aldoses 9a-d afforded the respective thiosemicarbazide derivatives. The manno-derivative 10, the D-galacto derivative 11 and the L-arabino derivative 12 exist in t Read More

Background: Aziridine compounds are among the most fascinating intermediates in organic synthesis, acting as precursors of many complex molecules due to the strain incorporated in their skeletons and can be opened in a stereo controlled manner with various nucleophiles, providing access to a wide range of important nitrogen-containing products. Sonochemistry involves the use of ultrasound technique to promote o Read More

Aim and Objective: Phosphonate possesses a broad range of applications ranging from agrochemistry to medicines. Because of the synthetic and biological importance of phosphonate, their chemistry has stimulated an increasing interest. Hence we developed an efficient and eco-friendly Mg(ClO4)2 catalyzed one pot, solvent free synthesis of phosphonate derivatives of chalcones. Materials and Methods: Magnesium perchl Read More