Category: 924818-16-6

In the chemical reaction process, reaction time, type of solvent, can easily affect the result of the reaction, thereby determining the yield and properties of the reaction product. An updated downstream synthesis route of 924818-16-6 as follows. Quality Control of (5-Chloro-2,4-difluorophenyl)methanamine

10489] A 50-mE 1-neck round bottom flask was charged with reactant 15-A (0.015 g, 0.047 mmol, the synthesis of 15-A is described in example 41), (5-chioro-2,4-difluorophe- nyl)methanamine (0.009 g, 0.05 mmol), DIPEA (0.06 g, 0.47 mmol) and HATU (0.035 g, 0.09 mmol) in DCM (3 ml). The reaction mixture was stirred at room temperature for 1 hout The reaction mixture was concentrated down, re-dissolved in EtOAc (50 mE), washed with saturated NaHCO3 twice, washed with saturated NH4C1 and dried over Na2 SO4. After concentration, the crude was purified by column chromatography on silica gel with hexane-EtOAc to obtain 15-B. ECMS-ESI (mlz): [M+H]. found: 483.

According to the analysis of related databases, 924818-16-6, the application of this compound in the production field has become more and more popular.

Reference:
Patent; Gilead Sciences, Inc.; Bacon, Elizabeth M.; Cai, Zhenhong R.; Cottell, Jeromy J.; Ji, Mingzhe; Jin, Haolun; Lazerwith, Scott E.; Morganelli, Philip Anthony; Pyun, Hyung-jung; (101 pag.)US2016/176870; (2016); A1;,
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

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;,
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Adding a certain compound to certain chemical reactions, such as: 924818-16-6, name is (5-Chloro-2,4-difluorophenyl)methanamine, belongs to chlorides-buliding-blocks compound, can increase the reaction rate and produce products with better performance than those obtained under traditional synthetic methods. Here is a downstream synthesis route of the compound 924818-16-6, Product Details of 924818-16-6

N-(5-Chloro-2,4-difluorobenzyl)-2,2-dimethoxyacetamide; A mixture of methyl dimethoxyacetate (1.45 g, 10.7 mmol) and 5-chloro-2,4-difluorobenzylamine (1.78 g, 10.0 mmol) in a sealed tube was heated at 80¡ã C. for 20 h. After that time, the mixture was diluted with EtOAc (20 ml), washed with HCl (2 N, 10 ml), saturated Na2CO3 (10 ml), H2O (10 ml) and brine (10 ml), and dried over MgSO4. After concentrated in vacuo, the title compound was obtained as a brown oil. 1H NMR (400 MHz, CDCl3): delta=3.41 (s, 6 H), 4.46 (d, J=6.4 Hz, 2H), 4.74 (s, 1H), 6.92 (t, J=8.8 Hz, 1H), 6.93 (brs, 1H), 7.41 (t, J=8.0 Hz, 1H). MS(ES+): m/z=280.03/282.01 (95/57) [MH+]. HPLC: tR=3.02 min (polar-5 min, ZQ3).

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Reference:
Patent; OSI Pharmaceuticals, Inc.; US2009/197862; (2009); A1;,
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics