Letters in Organic Chemistry - Volume 15, Issue 3, 2018

In the current research, a facile and green one pot synthesis of new gabapentin-lactams (G2-G8) has been achieved by reacting gabapentin (G1) with a variety of sulfonyl chlorides. The new lactamization protocol is furnished under the green solvent i.e., water and reaction was completed in a short period of time by just stirring at room temperature. Whereas in some cases, annulation could not happen and furnished un-cyclize Read More

Background: Chiral three-membered heterocycles occupy a special place in medicinal and pharmaceutical chemistry related to their diversity of biological activities due to the strain incorporated in their skeletons. This review covers developments reported in the last thirteen years in asymmetric epoxidation, aziridination, azirination and thiirination applied to the synthesis of biologically relevant or natural three-memb Read More

Background: The continued resistance of the body to antimicrobial drugs has led to the urgent need of preparing new heterogeneous compounds that are active antibacterial and antifungal. Methods: Two series of [1,2,4]triazolo[4,3-a]pyrimidines 8 and pyrido[3,2-f][1,4]thiazepines 12 were prepared in moderate to excellent yields through the reaction of pyrimidinethione 4 and pyridinethione 10 with the appropriate hydrazo Read More

Background: A number of protective groups for hydroxyl functional groups have been developed to date. Alcohols are most commonly protected as ethers and esters, where in alkyl and benzyl ethers are strong protective groups while others, like THP, TBS, TPS and MEM/MOM ethers are acid labile. Among all other hydroxyl protecting groups, Silyl ethers are the most frequently used protecting groups because they are easily a Read More

Background: Acylnitroso intermediates are considered as highly reactive and useful transient that have been used to synthesize a broad class of biological active compounds and synthetic drugs. Although there are some reported methods for the generation of these intermediates, but still challenge for mild and environmental benign protocol. Herein, we report the facile in situ synthesis of acylnitroso intermediates and thei Read More

Background#154;Several studies have shown excellent antitumor activity of erucin, but there are few studies on its analogues. The aim of the study involves the synthesis and the antitumor activities of novel erucin analogues. Ten novel erucin analogues were synthesized and evaluated for their efficacy as antitumor agents. Methods: Ten novel erucin analogues were synthesized by using 1, 4-dibromobutane and potassium p Read More

Background: Chitosan is well-known as a metal chelating agent for removing metal ions in near-neutral conditions. Chemical modification of chitosan has attracted attention to improve its metalion adsorbent properties. Recently, dibenzo-24-crown-8 derivatives were synthesized and reported to chelate with metal ions such as cesium. However, to date, to the best of our knowledge, there is no report on the use of dib Read More

Background: Euphorbia species are known for the diversity of terpenes, and the presence of toxic diterpenoids in Euphorbia species have raised occupational and eco-toxicological concerns. The present study reports the terpene profile of Euphorbia tortilis Rottler ex Ainslie, along with cytotoxicity assay. Method: Triterpenes were isolated from the hexane extract of E. tortilis through column chromatography and were ch Read More

Background: Pyrrole moiety is found in naturally occurring compounds such as chlorophyll, haem, and vitamin B12 and present in a number of drugs for example atorvastatin, ketorolac, elopiprazole, tolmetin and sunitinib. Various methods have been used for the synthesis of pyrrole derivatives; however, still there is a need for environmentally benign and economic protocol. Method: We have reported a simple, mild a Read More

Hydroxymethylfurfural (HMF) is one of the important parameters to determine the quality and freshness of honey relating to thermal treatment and storage condition, respectively. Many studies have been extensively carried out to investigate the effect of heating temperature and duration on the formation of HMF. These data were collected from literature, and critically analyzed using statistical techniques including multivar Read More