Liu, Ping et al. published their research in ACS Medicinal Chemistry Letters in 2018 | CAS: 852854-41-2

2-(Bromomethyl)-4-(trifluoromethyl)thiazole (cas: 852854-41-2) belongs to thiazole derivatives. The higher aromaticity of thiazole is due to delocalization of a lone pair of sulfur electrons across the ring, which is evidenced by chemical shifts of ring hydrogen at δ 7.27 and 8.77 ppm (C2 and C4), indicating diamagnetic ring current. The pyridine-type nitrogen in the thiazole ring deactivates the ring for electrophilic substitution reactions, which is further reduced in acid due to protonation of the thiazole ring.Quality Control of 2-(Bromomethyl)-4-(trifluoromethyl)thiazole

Discovery of orally bioavailable and liver-targeted hypoxia-inducible factor prolyl hydroxylase (HIF-PHD) inhibitors for the treatment of anemia was written by Liu, Ping;Wang, Liping;DuBois, Byron G.;Colandrea, Vincent J.;Liu, Rongqiang;Cai, Jiaqiang;Du, Xiaoxing;Quan, Weiguo;Morris, William;Bai, Jianwu;Bishwokarma, Bimjhana;Cheng, Mangeng;Piesvaux, Jennifer;Ray, Kallol;Alpert, Carla;Chiu, Chi-Sung;Zielstorff, Mark;Metzger, Joseph M.;Yang, Liming;Leung, Dennis;Alleyne, Candice;Vincent, Stella H.;Pucci, Vincenzo;Li, Xiaofang;Crespo, Alejandro;Stickens, Dominique;Hale, Jeffrey J.;Ujjainwalla, Feroze;Sinz, Christopher J.. And the article was included in ACS Medicinal Chemistry Letters in 2018.Quality Control of 2-(Bromomethyl)-4-(trifluoromethyl)thiazole The following contents are mentioned in the article:

We report herein the design and synthesis of a series of orally active, liver-targeted hypoxia-inducible factor prolyl hydroxylase (HIF-PHD) inhibitors for the treatment of anemia. In order to mitigate the concerns for potential systemic side effects, we pursued liver-targeted HIF-PHD inhibitors relying on uptake via organic anion transporting polypeptides (OATPs). Starting from a systemic HIF-PHD inhibitor (1), medicinal chem. efforts directed toward reducing permeability and, at the same time, maintaining oral absorption led to the synthesis of an array of structurally diverse hydroxypyridone analogs. Compound 28a was chosen for further profiling, because of its excellent in vitro profile and liver selectivity. This compound significantly increased Hb levels in rats, following chronic QD oral administration, and displayed selectivity over systemic effects. This study involved multiple reactions and reactants, such as 2-(Bromomethyl)-4-(trifluoromethyl)thiazole (cas: 852854-41-2Quality Control of 2-(Bromomethyl)-4-(trifluoromethyl)thiazole).

2-(Bromomethyl)-4-(trifluoromethyl)thiazole (cas: 852854-41-2) belongs to thiazole derivatives. The higher aromaticity of thiazole is due to delocalization of a lone pair of sulfur electrons across the ring, which is evidenced by chemical shifts of ring hydrogen at δ 7.27 and 8.77 ppm (C2 and C4), indicating diamagnetic ring current. The pyridine-type nitrogen in the thiazole ring deactivates the ring for electrophilic substitution reactions, which is further reduced in acid due to protonation of the thiazole ring.Quality Control of 2-(Bromomethyl)-4-(trifluoromethyl)thiazole

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica