Current Organic Synthesis - Online First

Background Timolol maleate is clinically used for the treatment of hypertension, angina pectoris, tachycardia, and glaucoma. Objective The aim of this study was to enhance the safe use of timolol maleate and investigate a synthesis method for 3-S-timolol, a newly identified impurity in timolol API (Active Pharmaceutical Ingredients). Methods (S)-3-(tert-butylamino)propane-1,2-diol (1) was used as a raw material. 3-S-timolol ma Read More

Introduction An efficient procedure was reported for the synthesis of novel hybrid dithiazoles 7 and thiazoles 15, in good yields, by applying hydrazonyl chlorides 4 with thiocarbohydrazone derivatives 3 and 12. Methods The thiazole derivatives were evaluated for their antimicrobial and antioxidant activities. Results According to the results, thiazoles revealed marked potency as antimicrobial and antioxidant agents. Thus, Read More

Introduction The origin, synthesis, characterization and docking studies of (Z)-7-((1R,2R,3R,5S)-3,5-dihydroxy-2-((R,1E,4E)-3-hydroxy-5-phenylpenta-1,4-dien-1-yl)cyclopentyl)-N-ethylhept-5-enamide, an impurity generated in the preparation of an anti-glaucoma agent-Bimatoprost has been described. Methods This impurity was controlled by employing 30% Pd/C, and the impurity level was brought to the permissible level, i.e. Read More

erivatives of pyrimidinone, dihydropyrimidinone, and 2,4-diaryl-substituted pyrimidines were synthesized by cyclocondensation of α-aminoamidines with various saturated carbonyl derivatives and their analogs. The therapeutic potential of the newly synthesized derivatives for cancer treatment was evaluated using molecular docking calculations. The molecular docking results indicate that some of the synthesized diaryl derivativ Read More

Introduction The protection of the hydroxyl group as formamides is a crucial initial step in pharmaceutical synthesis. Methods In this study, we investigated the O-formylation of alcohols using dimethylformamide (DMF) in a mixture with a new magnetic nanocomposite Fe3O4@Chitosan/POCl2-x. Results The results demonstrate that this core-shell heterogeneous nanocomposite facilitates the formation o Read More

The current review aimed to provide an understanding of the preparation, reactions, and biological action of thiazoles. The purpose of this review was to focus on the progress made in the synthesis of physiologically effective thiazole products with their interactions. A combinatorial approach was proposed, and extensive attempts were made in the search for thiazoles by chemists in many domains due to the information of m Read More