Extracurricular laboratory: Synthetic route of 57381-43-8

According to the analysis of related databases, 57381-43-8, the application of this compound in the production field has become more and more popular.

Application of 57381-43-8, 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 57381-43-8 as follows.

Step 3: Preparation of 5-Bromo-2-r3-cyclopropyl-l-(3-methyl-pyridin-2-yl)-lH-pyrazol-5- ylaminol-benzoic acid methyl ester; To a mixture of 3-cyclopropyl-l-(3-methyl-pyridin-2-yl)-lH-pyrazol-5-amine (1.0 g, 4.667 mmol) and 2,5-dibromo-benzoic acid methyl ester (1.25 g, 4.243 mmol) in toluene (20 mL) was added BINAP (0.264 g, 0.424 mmol), followed by Pd2(dba)3 (0.233 g, 0.255 mmol). To the mixture was added cesium carbonate (1.94 g, 5.94 mmol) and the suspension was heated at 118 ¡ãC overnight and cooled to rt. The cooled reaction mixture was diluted with ethyl acetate and filtered through Celite and concentrated. The product (0.61 g, 31percent) was isolated by column chromatography (25percent ethyl acetate/ hexanes), then on the HPLC (20 to 90 percent acetonitrile). MS m/z 427.1 (M+); HPLC RT (min) 4.06 {method (A)}.

According to the analysis of related databases, 57381-43-8, the application of this compound in the production field has become more and more popular.

Reference:
Patent; BAYER PHARMACEUTICALS CORPORATION; WO2007/27842; (2007); A1;,
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics