Letters in Organic Chemistry - Volume 19, Issue 1, 2022

An unprecedented copper-catalyzed reaction of acetylene analogs with dialkyl azo dicarboxylate and benzazole analogs via a cross-coupling sequence was reported. A library of triazolobenzazole fused ring systems including [1,2,3] triazolo [3,4-b] [1,3] benzothiazole, [1,2,3] triazolo [3,4-b] [1,3] benzoxazole and [1,2,3] triazolo[3,4-b][1,3]benzimidazole structures were obtained in moderate to excellent yields under very mild Read More

An efficient methodology for the synthesis of 1,3-thiazolidin-4-ones using L-Proline as catalyst under aqueous conditions has been developed. The one-pot, multicomponent reaction of aromatic/ heterocyclic aldehyde, aromatic amine and thioglycolic acid at room temperature give 1,3- thiazolidin-4-ones in moderate to good yields. Further, the current approach is notably greener than traditional methods, with an E-facto Read More

Zn(OAc)2•2H2O-catalyzed one-pot multicomponent reaction of Betti bases using β- naphthol, aldehydes, and amines, under neat conditions in moderate to excellent yields (68- 96%) is reported in this study. This synthetic protocol offers several advantages, such as operational simplicity, shorter reaction period, high yields, and easy work-up procedures.

In this study, naturally occurring clay halloysite has been used to synthesize novel halloysite functionalized sulfonic acid in two steps, i.e. functionalization followed by oxidation, and its catalytic activity has been estimated for one-pot synthesis of Hantzsch 1,4-dihydropyridines under green solventfree conditions. Spectroscopic studies such as FTIR, TGA, elemental analysis and first-principles-based quantum chemical s Read More

An efficient method for the Sonogashira coupling reaction between aryl halides and terminal alkynes has been developed. The reaction was performed in ionic liquid 1-butyl-3- methylimidazolium tetrafluoroborate ([Bmim][BF4]) under microwave irradiation. High yields of products were obtained in a very short reaction time. Moreover, the medium and catalyst could be recovered and reused three times without consider Read More

A novel series of diimino dihydroquinazoline derivatives were synthesized from isocyanides and guanidine analogs in quantitative yields by applying an efficient, inexpensive, one-pot copper-catalyzed intramolecular C-H activation reaction under mild conditions. The structures were confirmed on the basis of IR, 1HNMR, 13C NMR, mass spectral and elemental analysis data. The protocol offers advantages like short reaction time, a Read More

The synthesis of axially chiral compounds has attracted a great deal of attention in recent years. Herein, an efficient and economical synthetic route has been developed for 2-(3- carbamoylpyridin-2-yl) nicotinamide pyridine salts, axially chiral compounds. The starting material 1,10-phenanthroline is readily available. In this study, 2-(3-carbamoylpyridin-2-yl) nicotinamide pyridine salts are obtained in moderate to goo Read More

The catalytic display of supported heterogeneous catalysts is essentially reliant on their constitutive elements, including active species and supports. Accordingly, the scheme and development of active catalysts with synergistically enhanced outcomes between active sites and supports are of high importance. A simple NaBH4 reduction method was used to synthesize cylindrical amine-functionalized silica nanotubes supp Read More

An efficient synthetic route for the novel bis-imdizo[1,2-a]pyridine-3-yl)methane (2a-k) derivatives have been developed using acetic acid and two drops of trifluoroacetic acid at 40-45oC, resulting in 60-72% yields. An attempt to synthesize bis(Imidazo[1,2-a]pyridin-3-yl)methyl chloride derivatives by the reaction between two moles of imidazo[1,2-a]pyridine, one mole of chloroacetaldehyde in acetic acid, and two drops Read More

A novel, mild and efficient protocol to synthesize dibrominated propanamides has been developed. The presented methodology provides several merits, such as easy-to-handle and stable brominated substrate, catalyst-free, additive-free, and facile experimental operation. The study on the preliminary mechanism indicated that a free radical pathway might be involved in the presented reaction.

The novel synthetic route to the antipsychotic drug Cariprazine was developed and demonstrated on a commercial scale. The synthesis of Cariprazine is achieved from N-(4- oxocyclohexyl) acetamide by using various reactions such as Wittig-Horner reaction, reduction of alkene, hydrolysis of ester, deacylation, amidation, reduction of Weinreb amide to yield the corresponding aldehyde, and finally reductive amina Read More

A Dansyl functionalized fluorescent probe (DFFP) has been intended, synthesized, and well-characterized (NMR, IR, Mass, SEM, SCXRD), capable of sensing trace amounts of water contaminant in hygroscopic deuterated solvents by changing colour under UV irradiation. A distinct bathochromic shift in emission spectra of probe DFFP and the visual colour change (Green to Yellow) under UV lamp are the key evidence of the prese Read More

Background: Schizophrenia is a severe mental disorder that affects around 1% of the population worldwide. The available antipsychotics alleviate the positive symptoms of the illness. However, their effect on the negative and cognitive symptoms is limited. The fruit powder of Terminalia bellerica has been found to possess antipsychotic activity, which might be useful in treating the symptoms of schizophrenia. Objective: T Read More