In 2010,Sidduri, Achyutharao; Grimsby, Joseph S.; Corbett, Wendy L.; Sarabu, Ramakanth; Grippo, Joseph F.; Lou, Jianping; Kester, Robert F.; Dvorozniak, Mark; Marcus, Linda; Spence, Cheryl; Racha, Jagdish K.; Moore, David J. published 《2,3-Disubstituted acrylamides as potent glucokinase activators》.Bioorganic & Medicinal Chemistry Letters published the findings.HPLC of Formula: 3034-22-8 The information in the text is summarized as follows:
The phenylacetamide 1 represents the archtypical glucokinase activator (GKA) in which only the R-isomer is active. In order to probe whether the chiral center could be replaced, we prepared a series of olefins 2 and show in the present work that these compounds represent a new class of GKAs. Surprisingly, the SAR of the new series paralleled that of the saturated derivatives with the exception that there was greater tolerance for larger alkyl and cycloalkyl groups at R2 region in comparison to the phenylacetamides. In normal Wistar rats, the 2,3-disubstituted acrylamide analog 10 was well absorbed and demonstrated robust glucose lowering effects. The experimental part of the paper was very detailed, including the reaction process of 5-Bromothiazol-2-amine(cas: 3034-22-8HPLC of Formula: 3034-22-8)
5-Bromothiazol-2-amine(cas: 3034-22-8) belongs to anime. Nitrous acid converts secondary amines (aliphatic or aromatic) to N-nitroso compounds (nitrosamines): R2NH + HNO2 → R2N―NO. Some nitrosamines are potent cancer-inducing substances, and their possible formation is a serious consideration when nitrites, which are salts of nitrous acid, are present in foods or pharmaceutical preparations. Tertiary amines give rise to nitrosamines more slowly; an alkyl group is eliminated as an aldehyde or ketone, along with nitrous oxide, N2O.HPLC of Formula: 3034-22-8
Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica