In 2010,Pan, Shifeng; Wu, Xu; Jiang, Jiqing; Gao, Wenqi; Wan, Yongqin; Cheng, Dai; Han, Dong; Liu, Jun; Englund, Nathan P.; Wang, Yan; Peukert, Stefan; Miller-Moslin, Karen; Yuan, Jing; Guo, Ribo; Matsumoto, Melissa; Vattay, Anthony; Jiang, Yun; Tsao, Jeffrey; Sun, Fangxian; Pferdekamper, AnneMarie C.; Dodd, Stephanie; Tuntland, Tove; Maniara, Wieslawa; Kelleher, Joseph F. III; Yao, Yung-mae; Warmuth, Markus; Williams, Juliet; Dorsch, Marion published 《Discovery of NVP-LDE225, a Potent and Selective Smoothened Antagonist》.ACS Medicinal Chemistry Letters published the findings.Synthetic Route of C8H7BrO2 The information in the text is summarized as follows:
The blockade of aberrant hedgehog (Hh) signaling has shown promise for therapeutic intervention in cancer. A cell-based phenotypic high-throughput screen was performed, and the lead structure (1) was identified as an inhibitor of the Hh pathway via antagonism of the Smoothened receptor (Smo). Structure-activity relation studies led to the discovery of a potent and specific Smoothened antagonist N-(6-((2S,6R)-2,6-dimethylmorpholino)pyridin-3-yl)-2-methyl-4′-(trifluoromethoxy)biphenyl-3-carboxamide (5m, NVP-LDE225), which is currently in clin. development. In the experiment, the researchers used 3-Bromo-2-methylbenzoic acid(cas: 76006-33-2Synthetic Route of C8H7BrO2)
3-Bromo-2-methylbenzoic acid(cas: 76006-33-2) belongs to organobromine compounds.The reactivity of organobromine compounds resembles but is intermediate between the reactivity of organochlorine and organoiodine compounds. Synthetic Route of C8H7BrO2 The principal reactions for organobromides include dehydrobromination, Grignard reactions, reductive coupling, and nucleophilic substitution.
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary