Letters in Organic Chemistry - Volume 14, Issue 10, 2017

Combination of urea hydrogen peroxide and p-toluenesulfonyl chloride in methanol was proved to be facile and highly efficient for the oxidative methyl esterification of various aldehydes to the corresponding carboxylic methyl esters.

Background: Heterocycles are the gold mines in medicinal chemistry. Most drugs used in today's medicinal period possess a heterocyclic nucleus. One of the interesting heterocycles, benzothiazole, a potent phamacophore, is highly important in the medicinal chemistry due to its association with diverse pharmacological properties. Development in biological evaluation of heterocyclic molecule has undergone manifold change Read More

A series of lupane C19-(1,2,3-triazolyl)-triterpenoids were obtained by “click” reaction of 3,28-diacetoxy-29-norlup- 20(30)-yne with different aromatic and sugar azides after screening of several copper-based catalytic systems. DFT calculations were performed (B3LYP/6.311 level of theory) and showed that the alkyne moiety is hindered by the triterpenoid skeleton, thus explaining its low reactivity and the requiremen Read More

Background: The 4-benzyl biphenyl scaffold represents an important structural element widely used in optoelectronic materials and bioactive compounds, including a variety of antihypertensive drugs and prostate cancer agents. Therefore, the construction of 4-benzyl groups incorporating this structural feature with cheap and readily available starting materials is of great scientific interest. Methods: In this paper, the reduct Read More

Thieno[3,2-b]thiophene represents a typical core structure in a large number of organic optoelectronic materials and molecular magnetism. One-pot efficient approach to modify the electronic structure of thieno[3,2-b]thiophene is to introduce suitable substituents into this π- conjugated skeleton. In this paper, we report on a facile route to precisely functionalize thieno[3,2- b]thiophene by the direct Pd-catalyzed arylation Read More

Background: Amide bond is prevalent in peptides. Moreover, at least 25% pharmaceutical products also contain amide bond. A wide ranging strategy including Ugi reaction and related multicomponent reactions is available for the synthesis of amide. While HATU mediated direct one-pot diamide synthesis is scarcely investigated in the literature. Objective: The objective of this work is to achieve a one pot synthesis of diam Read More

Background: Clobazam (CLB) has been used as an anxiolytic, anticonvulsant and antiepileptic drug under the trade names, Frisium, Urbanol, Onfi and Tapclob. Impurity profiling in the pharmaceutical industries is a central task in the manufacturing of drug product. The quantification of impurities in active pharmaceutical ingredients (APIs) is also receiving considerable importance from the regulatory authorities in the po Read More

Background: Proline and its derivatives are versatile organocatalysts for many reactions. Especially prolinamide derivatives have been prepared and investigated in aldol reaction successfully. Generally, derivatizations have been made on side chain of proline to develop new effective catalysts. But, there are only few examples of different cyclic systems other than pyrrolidine ring used as chiral organocatalysts. Method Read More

Background: Polyhydroquinoline derivatives are known as one of the most significant class of biologically active heterocycles. Herein, in this paper, magnetite polycitric acid (Fe3O4@PCA) nanoparticles as novel, efficient and reusable catalysts were used for the preparation of polyhydroquinoline derivatives. Method: Using aromatic and heteroaryl aldehydes with dimedone, ammonium acetate and ethyl acetoacetate, polyhydroqui Read More