Letters in Organic Chemistry - Volume 16, Issue 1, 2019

PF-543 has been known as a substance that strongly inhibits SK1. However, it also exhibits antineoplastic activity that is lower than other inhibitors of SK1. In this study, we compared PF-543 and synthesized a newly designed derivative of PF-543 (compound 2) in which two aromatic structures were connected in para-form. The synthesized derivative showed inhibitory effect on SK1, similar to that of PF-543. However, it was mor Read More

Acetanilide or N-phenylacetamide is an aromatic compound having phenyl ring attached to an acetamido group (–NHCOCH3). In 1886, acetanilide was introduced as an analgesic and antipyretic drug into medical practice by A. Cahn and P. Hepp. Since then, many acetanilide derivatives have been found to have antimicrobial, analgesic, anti-inflammatory, antipyretic, antioxidant, anticonvulsant, anti- cancer, antihyperglycaemi Read More

Efficient C-S and C-N cross-coupling reactions have been developed for regioselective, scalable and environmentally benign synthesis of substituted phenothiazine derivatives. Cross-coupling reactions were demonstrated on various challenging substrates using non-toxic, highly economical, readily available ferric citrate as a catalyst to get desired product with high regioselectivity. Atom economy is the added advantage of th Read More

Starting from 2,3-dichloroquinoxaline, a synthetic strategy for the preparation of 1-(3- phenylpropyl)-4-(pyridinylmethoxy)[1,2,4]triazolo[4,3-a]quinoxalines is described.

A new phosphonium based coupling reagent DEPO-B has been synthesized from 5- (hydroxyimino)-1,3-dimethylpyrimidine-2,4,6 (1H,3H,5H)-trione (Oxyma B) and diethyl chlorophosphate in presence of base. It is a solid material and the hydrolytic stability and solubility was evaluated for confirming its capability for usage in automated peptide synthesizer.

CDI combined with CH3SO3H was found to be highly effective for the cyclization of 2-aminothiophenol derivatives with carboxylic acids under MW condition. Fourteen benzothiazole derivatives were synthesized in good yield and their structures were characterized by 1H-NMR, 13CNMR, IR and mass spectrometry. This simple, rapid synthetic method is believed to provide a useful process for the synthesis of 2-substituted benzoth Read More

In the present paper, synthesis of few novel pregnane derivatives and their evaluation as potential anti-hyperlipidemic and anti-oxidant agents has been reported. The synthesis of 3β-hydroxy- 16α-methoxy pregn-5-en-20-one (4) was achieved by reaction of 3β-hydroxy-5,16-pregnadiene-20-one (3) with KOH/MeOH under reflux. Compound 4 on treatment with succinic and phthalic anhydride afforded compound 6 and 7, respectiv Read More

The present study aimed to investigate the chemical constituents, and antioxidants and antitumor activities of the seagrasses Halodule uninervis and Thalassia hemprichii. Seventeen compounds were isolated from both seagrasses, and identified as flavonoids, phenolic acids, nitrogen compound, steroids and fatty acids. Their structures were established by spectral analysis (UV, MS, and 1D- and 2D-NMR) and chemical i Read More

An efficient catalytic synthesis of 4-aryl-3,4-dihydropyrimidine-2(1H)-one derivatives using copper (II), iron (III) and zinc (II) exchanged montmorillonite clays as a catalyst is described. The desired products were obtained in good yields.

In this study, we describe a microwave-based click chemistry method used to prepare a family of novel bis-flavone dimers. The substituted 7-hydroxy and 4’-hydroxy flavonoids were linked through a triazole ring. The compounds were easily synthesized and purified in high yields. The bisflavonoids were tested on different cell lines including HCT116, HepG2, MCF7 and MOLT-4. Several analogues showed to have antican Read More

Phosphazene bases have been utilized as efficient organocatalysts to catalyze the double Michael additions of divinyl ketones with active methylenes to afford functionalized cyclohexanones in 36-91% yields with >25:1 diastereoselectivity.