The pyrimidine ring system has wide occurrence in nature as substituted and ring fused compounds and derivatives, including the nucleotides cytosine, thymine and uracil, thiamine (vitamin B1) and alloxan. 2927-71-1, formula is C4HCl2FN2, Name is 2,4-Dichloro-5-fluoropyrimidine. It is also found in many synthetic compounds such as barbiturates and the HIV drug, zidovudine. Synthetic Route of 2927-71-1.
Huang, Wei-Sheng;Liu, Shuangying;Zou, Dong;Thomas, Mathew;Wang, Yihan;Zhou, Tianjun;Romero, Jan;Kohlmann, Anna;Li, Feng;Qi, Jiwei;Cai, Lisi;Dwight, Timothy A.;Xu, Yongjin;Xu, Rongsong;Dodd, Rory;Toms, Angela;Parillon, Lois;Lu, Xiaohui;Anjum, Rana;Zhang, Sen;Wang, Frank;Keats, Jeffrey;Wardwell, Scott D.;Ning, Yaoyu;Xu, Qihong;Moran, Lauren E.;Mohemmad, Qurish K.;Jang, Hyun Gyung;Clackson, Tim;Narasimhan, Narayana I.;Rivera, Victor M.;Zhu, Xiaotian;Dalgarno, David;Shakespeare, William C. research published ã?Discovery of Brigatinib (AP26113), a Phosphine Oxide-Containing, Potent, Orally Active Inhibitor of Anaplastic Lymphoma Kinaseã? the research content is summarized as follows. In the treatment of echinoderm microtubule-associated protein-like 4 (EML4)-anaplastic lymphoma kinase pos. (ALK+) non-small-cell lung cancer (NSCLC), secondary mutations within the ALK kinase domain have emerged as a major resistance mechanism to both first- and second-generation ALK inhibitors. This report describes the design and synthesis of a series of 2,4-diarylaminopyrimidine-based potent and selective ALK inhibitors culminating in identification of the investigational clin. candidate brigatinib. A unique structural feature of brigatinib is a phosphine oxide, an overlooked but novel hydrogen-bond acceptor that drives potency and selectivity in addition to favorable ADME properties. Brigatinib displayed low nanomolar IC50s against native ALK and all tested clin. relevant ALK mutants in both enzyme-based biochem. and cell-based viability assays and demonstrated efficacy in multiple ALK+ xenografts in mice, including Karpas-299 (anaplastic large-cell lymphomas [ALCL]) and H3122 (NSCLC). Brigatinib represents the most clin. advanced phosphine oxide-containing drug candidate to date and is currently being evaluated in a global phase 2 registration trial.
Synthetic Route of 2927-71-1, 2,4-Dichloro-5-fluoropyrimidine is a useful research compound. Its molecular formula is C4HCl2FN2 and its molecular weight is 166.97 g/mol. The purity is usually 95%.
2,4-Dichloro-5-fluoropyrimidine is an aromatic hydrocarbon that has been shown to inhibit the growth of mouse tumor cells in vitro. It also inhibits the production of amines by reacting with industrial chemicals and sodium carbonate. This compound has potent inhibitory activity against autoimmune diseases and cytotoxic potency on mcf-7 cells. Furthermore, 2,4-Dichloro-5-fluoropyrimidine has been shown to have a chlorinating effect on cancer cells., 2927-71-1.
Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia