Extended knowledge of 578008-32-9

According to the analysis of related databases, 578008-32-9, the application of this compound in the production field has become more and more popular.

Synthetic Route of 578008-32-9, 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 578008-32-9 as follows.

Typical procedure for the Buchwald reaction with terf-butoxycarbonyl protected pyrazole:2-(2-Chloro-4-trifluoromethyl-phenyl)-4-(5-methyl-lH-pyrazol-3-ylamino)-2H- phthalazin- 1 -one4-Bromo-2-(2-cUoro-4-trifluoromethyl-phenyl)-2H-phthalazin-l-one (obtained from the above phthalazine-l,4-dione by bromination with POBr3 in analogy to Method R, as reported above) (0.15g, 0.37mmol), 3-amino-5-methyl-pyrazole-l- carboxylic acid tert-butyl ester (0.08Og, 0.41mmol), Cs2CO3 (0.033g, 0.34mmol), tris-(dibenzylideneacetone)-dipalladium (0.017g, 0.019mmol) and 4,5- bis(diphenylphosphino)-9,9-dimethylxanthene (0.022g, 0.037mmol) in 2 ml dry dioxane under nitrogen were heated to 100C for 18 hours, and then allowed to cool to room temperature. H2O was added and the solvent was evaporated in vacuum. The resulting solid was collected by filtration. Purification of the raw product by preparative HPLC gave the title compound (0.069g, 44% yield). 1H- EPO NMR: (400 MHz, D6-DMSO) 11.92 (IH, s), 9.34 (IH, s), 8.54 (IH, d), 8.35 (IH, d), 8.14 (IH, s), 8.01 (IH, t), 7.92 (3H, m), 6.06 (IH, s), 2.14 (3H, s); MS (ESI+) = 420.23 (M+H)+.

According to the analysis of related databases, 578008-32-9, the application of this compound in the production field has become more and more popular.

Reference:
Patent; F. HOFFMANN-LA ROCHE AG; WO2006/32518; (2006); A1;,
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics