Analyzing the synthesis route of 1029721-02-5

The basis of chemical reaction formula synthesis, the synthesis route is composed of some specific reactions and combined according to certain logical thinking. We look forward to the emergence of more reaction modes in the future.

Researchers who often do experiments know that organic synthesis is a process of preparing more complex target molecules from simple raw materials through one or more chemical reactions. Generally, it requires fewer steps, and cheap raw materials. 1029721-02-5, name is 4-Oxo-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrazine-2-carboxylic acid, A new synthetic method of this compound is introduced below., category: Pyrazines

To a suspension of 4,5,6, 7-tetrahydro-4-oxo-pyrazolo[1 ,5-a]pyrazine-2 carboxylic acid (181 mg, 1.0 mmol) in THF (15 mL) was added diphenylphosphoryl azide (0.25 mL, 1.0 mmol) and Et3N (0.28 mL. 2.0 mmol) The resulting mixture was heated to reflux for 6 h and cooled to room temperature. Then 6-fluoro-1-(piperidin-4-yl)indoline (88 mg, 0.4 mmol) and Et3N (0.14 mL, 1.0 mmol) were added sequentially. The resulting mixture was stirred at room temperature for 24 h and concentrated. The resulting residue was purified by chromatography using EtOAc, then 2-5% MeOH/EtOAc as the eluent to yield 4-(6-fluoroindolin-1-yl)-N-(4-oxo-4,5,6,7-tetrahydropyrazolo[1 ,5- a]pyrazin-2-yl)piperidine-1-carboxamide.

The basis of chemical reaction formula synthesis, the synthesis route is composed of some specific reactions and combined according to certain logical thinking. We look forward to the emergence of more reaction modes in the future.

Reference:
Patent; JANSSEN PHARMACEUTICA NV; YANG, Shyh-Ming; KUO, Gee-Hong; GAUL, Micheal, D.; RANO, Thomas, A.; WO2013/85954; (2013); A1;,
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem