Process for preparing 5-fluoro-1h-pyrazolo [3, 4-b]...

Details Process for preparing 5-fluoro-1h-pyrazolo [3, 4-b]... Process for preparing 5-fluoro-1h-pyrazolo [3, 4-b]...

C - Chemistry, Metallurgy

07

D

C07D 471/04 (2006.01)

Patent

CA 2694499

The present invention relates to a process for the synthesis of 5-fluoro-1H- pyrazolo [3, 4-b]pyridin-3-amine in high yield and purity. The present invention also relates to processes for the synthesis of 5-fluoro-1H-pyrazolo [3, 4- b] pyridin-3-amine derivatives. These processes are useful for preparing biologically active compounds, particularly certain GSK-3 inhibitors, or deriva-tives thereof. Reagents and conditi ons : i. Pd ( OAc )2, PPh3, Et3N, H2CO2; i i. 1 )(COCl)2, CH2Cl2, cat. DMF; 2 ) NH3 (g ), dioxane, i i i. TFAA, Et3N, CH2Cl2, O°C; iv. H2NNH2. H2O, n-butanol, reflux.

La présente invention concerne un procédé de synthèse de la 5-fluoro-1H-pyrazolo[3,4-b]pyridin-3-amine à rendement et pureté élevés. La présente invention concerne également des procédés de synthèse de dérivés de 5-fluoro-1H-pyrazolo[3,4-b]pyridin-3-amine. Ces procédés permettent de préparer des composés biologiquement actifs, en particulier certains inhibiteurs GSK-3, ou des dérivés de ceux-ci. Réactifs et conditions : i. Pd (OAc)2, PPh3, Et3N, H2CO2 ; ii. 1) (COCl)2, CH2Cl2, cat. DMF ; 2) NH3 (g ), dioxane, iii. TFAA, Et3N, CH2Cl2, O°C ; iv. H2NNH2. H2O, n-butanol, reflux.

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