Related Products of 924818-16-6,Some common heterocyclic compound, 924818-16-6, name is (5-Chloro-2,4-difluorophenyl)methanamine, molecular formula is C7H6ClF2N, traditional synthetic route has been very mature, but the traditional synthetic route has various shortcomings, such as complicated route, low yield, poor purity, etc, below Introduce a new synthetic route.
Example 80 Preparation of Compound 8Theta (1 R,4S, 12a )-N-(5-chloro-2,4-difluorobenzyl)-7-hydroxy-6,8-dioxo- 1 ,2,3,4,6,8, 12,12a- octahydro-l ,4-methanodipyrido[l ,2-a: r,2′-d]pyrazine-9-carboxamide 80 Step 1 A 50-mL round bottom flask was charged with 80-A (0.12 g, 0.32 mmol), (5-chloro-254-difluorophenyl)methanamme (0.1. 1 g, 0.63 mmol), N,N~ diisopropylethy famine (DIPEA) (0.20 g, 1.58 mmol) and HATU (0.24 g, 0.63 mmol) in EX 1 ( .10 ml). The reaction mixture was stirred at room temperature for 1 h. The reaction mixture was concentrated down, re-dissolved in EtOAc (50 raL), washed with saturated NaHCOj (2x), saturated NH4CI and dried over Na2S04. After concentration, the crude was purified by column chromatography on silica gel with hexane-EtOAc to obtain 80-B as a white solid. LCMS-ES ini/z): j VI · i | ; found: 541 .
These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route (5-Chloro-2,4-difluorophenyl)methanamine, its application will become more common.
Reference:
Patent; GILEAD SCIENCES, INC.; JIN, Haolun; LAZERWITH, Scott, E.; MARTIN, Teresa, Alejandra, Trejo; BACON, Elizabeth, M.; COTTELL, Jeromy, J.; CAI, Zhenhong, R.; PYUN, Hyung-Jung; MORGANELLI, Philip, Anthony; JI, Mingzhe; TAYLOR, James, G.; CHEN, Xiaowu; MISH, Michael, R.; DESAI, Manoj, C.; WO2014/100323; (2014); A1;,
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