These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route 64517-88-0, its application will become more common.
Some common heterocyclic compound, 64517-88-0, name is 1,3-Dimethyl-1H-pyrazol-4-amine, molecular formula is C5H9N3, 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. Quality Control of 1,3-Dimethyl-1H-pyrazol-4-amine
Example 4.28 7- [ [2- [(1 ,3-Dimethylpyrazol-4-yl)aminol -5-fluor o-4-pyridvH aminol -4-(4- isopropylpiperazin-l-yl)-2-methyl-isoindolin-l-one A mixture of 7-[(2-chloro-5-fluoropyridin-4-yl)amino]-2-methyl-4-(4-propan-2- ylpiperazin-l-yl)-3H-isoindol-l-one (150 mg, 0.36 mmol), l,3-dimethylpyrazol-4-amine (80 mg, 0.72 mmol), cesium carbonate (234 mg, 0.72 mmol), 9,9-dimethyl-4,5- bis(diphenylphosphino)xanthene (24.92 mg, 0.04 mmol) and palladium(II) acetate (6.45 mg, 0.03 mmol) was suspended in DMA (2 mL) under an atmosphere of nitrogen. The mixture was heated at 1500C for 60 minutes in a microwave reactor and then allowed to cool to room temperature. The mixture was filtered and the filtrate evaporated. The residue was dissolved in MeOH (20 mL) and the solution made acidic (pH6) by the addition of 2M HCl. The mixture was loaded onto an SCX column and the product eluted first wit MeOH and then with a 0.7M solution OfNH3 in MeOH. Fractions containing product were combined and evaporated and the residue was then purified by preparative HPLC. Fractions containing product were combined and evaporated to afford example 4.28 (45.4 mg, 26% yield); 1H NMR spectrum (300 MHz, DMSO): delta 1.02 (6H, d), 2.11 (3H, s), 2.60 (4H, t), 2.70 (IH, m), 2.99 (4H,m), 3.06 (3H, s), 3.70 (3H, s), 4.48 (2H, s), 6.92 (IH, d), 7.15 (IH, d), 7.39 (IH, d), 7.86 – 7.93 (3H, m), 9.26 (IH, d); Mass spectrum: m/z (ESI+) (M+H)+ = 493.44.
These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route 64517-88-0, its application will become more common.
Reference:
Patent; ASTRAZENECA AB; ASTRAZENECA UK LIMITED; WO2009/153589; (2009); A1;,
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics