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Asymmetric synthesis of aziridine with a new catalyst can help develop novel medicines

 E-Mail IMAGE: Scientists from Japan recently proposed a possible transition state for the reaction between aziridines and oxazolones in presence of a cinchona alkaloid sulfonamide catalyst, producing desirable aziridine-oxazolone compounds with high. view more  Credit: Image courtesy: Shuichi Nakamura from NITech Unless you ve studied chemistry in college, it s unlikely you ve come across the name aziridine. An organic compound with the molecular formula, C2H4NH, aziridines are well-known among medicinal chemists, who make use of the compound to prepare pharmaceutical drugs such as Mitomycin C, a chemotherapeutic agent known for its anti-tumor activity. Specifically, aziridines are what chemists call enantiomers molecules that are mirror images of each other and cannot be superposed on one another. A peculiarity with enantiomers is that the biological activity of one is different from its mirror image and only one of them is desirable for making drugs. Chemists, ther

New method of producing drug candidates may lead to better medicines in the future

New method of producing drug candidates may lead to better medicines in the future A lot of our medicines and other bioactive drugs are based on chemical structures called enantiomers molecules that are mirror images of each other and are non-superimposable. Notable among them are chiral N,N-acetals contained in diuretic drugs like bendroflumethiazide and thiabutazide, used to treat high blood pressure and edema. Because an enantiomer and its mirror image version often have different biological activities, with only one of them having pharmacological utility, an enantioselective or asymmetric synthesis yielding the desired enantiomer in greater amounts is highly desirable.

New method for asymmetric N,N-acetal synthesis promises advances in drug development

 E-Mail IMAGE: A possible mechanism for the formation of chiral N,N-acetal via reaction between 2-aminobenzamide and α-ketoester in presence of chiral bis(imidazoline)-phosphoric acid catalyst view more  Credit: Picture courtesy: Shuichi Nakamura from NITech A lot of our medicines and other bioactive drugs are based on chemical structures called enantiomers molecules that are mirror images of each other and are non-superimposable. Notable among them are chiral N,N-acetals contained in diuretic drugs like bendroflumethiazide and thiabutazide, used to treat high blood pressure and edema. Because an enantiomer and its mirror image version often have different biological activities, with only one of them having pharmacological utility, an enantioselective or asymmetric synthesis yielding the desired enantiomer in greater amounts is highly desirable.

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