Application of 851984-15-1, With the rapid development and complex challenges of chemical substances, the synthesis of new drugs is usually one of the most effective ways to increase yield.851984-15-1, name is 6-Chloro-5-fluoropyrimidin-4-amine, molecular formula is C4H3ClFN3, molecular weight is 147.54, as common compound, the synthetic route is as follows.
To a solution of trans-3 -((3 -chloro-S-(trifluoromethyl)phenyl)amino) -2-oxo- [1,3 ?-bipiperidine] -4?-carboxamide 13 (42 mg, 0.10 mmol, 1.0 equiv) in 1-butanol (2 mL), 6-chloro-S-fluoropyrimidin-4-amine (18 mg, 0.12 mmol, 1.2 equiv) was added DIPEA (26 mg, 0.20 mmol, 2.0 equiv). The reaction solution was stirred at 120 C for 16 h. The mixture was diluted with EtOAc (20 mL), washed with H20 (10 mL) and brine (10 mL), dried (Na2504), filtered, and concentrated in vacuo. The crude was by purified by pre-HPLC (MeOHIH2O with 0.05% TFA as mobile phase) to give the compound (trans)- 1 ?-(6-amino-S -fluoropyrimidin-4-yl)-3 -((3 -chloro-S – (trifluoromethyl)phenyl)amino)-2-oxo-[ 1,3 ?-bipiperidine] -4?-carboxamide 14 (44 mg, yield:83%) as a yellow solid. ESI-MS (M+H) : 530.0. HPLC: (214 nm: 100%, 254 nm: 100%). ?H NMR (400 MHz, CD3OD) 5: 7.97 (s, 1H), 6.84 (s, 1H), 6.81 (s, 1H), 6.76 (s, 1H), 4.58-4.52 (m, 2H), 4.09-4.03 (m, 1H), 3.52-3.35 (m, 3H), 3.29-3.27 (m, 4H), 3.12-3.05 (m, 1H), 2.24-2.17 (m,1H), 2.02-1.91 (m, 3H), 1.80-1.63 (m, 2H).
Statistics shows that 851984-15-1 is playing an increasingly important role. we look forward to future research findings about 6-Chloro-5-fluoropyrimidin-4-amine.
Reference:
Patent; BIOGEN MA INC.; SUNESIS PHARMACEUTICALS, INC.; MACPHEE, J. Michael; NEUMAN, Linda L.; (89 pag.)WO2018/17153; (2018); A1;,
Pyrimidine | C4H4N2 – PubChem,
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