947249-01-6 (2-氨基-3-三氟甲基吡啶-5-硼酸频哪醇酯,5-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)-3-(trifluoromethyl)pyridin-2-amine)

_97%

反应条件：

1.1 Reagents: Potassium acetate Catalysts: Dichloro[1,1′-bis(diphenylphosphino)ferrocene]palladium(II) dichloromethane addu… Solvents: 1,4-Dioxane ; 25 - 30 °C; 30 °C → 100 °C; 15 - 16 h, 95 - 100 °C

参考文献：

Process for the preparation of a substituted imidazo[4,5-c]quinoline compound and its use for the treatment of cancer

, World Intellectual Property Organization, , ,

合成路线：1 步

_94%

反应条件：

1.1 Reagents: Potassium acetate Catalysts: Dichloro[1,1′-bis(diphenylphosphino)ferrocene]palladium(II) dichloromethane addu… Solvents: 1,4-Dioxane ; 10 h, rt → 100 °C

参考文献：

Preparation of pyridinyltriazoloquinoxaline derivatives and analogs for use as PI3K inhibitors

, World Intellectual Property Organization, , ,

合成路线：1 步

_84%

反应条件：

1.1 Reagents: Potassium acetate Catalysts: [1,1′-Bis(diphenylphosphino)ferrocene]dichloropalladium Solvents: 1,2-Dimethoxyethane ; 2 h, 80 °C

参考文献：

Preparation of heterocycles as mTOR and/or PI3 kinase inhibitors

, China, , ,

合成路线：1 步

_84%

反应条件：

1.1 Reagents: Potassium acetate Catalysts: [1,1′-Bis(diphenylphosphino)ferrocene]dichloropalladium Solvents: 1,2-Dimethoxyethane ; 30 °C → 80 °C; 2 h, 80 °C

参考文献：

Preparation of imidazoquinoline derivatives as inhibitors of mTOR and/or PI3K kinase

, China, , ,

合成路线：1 步

_72%

反应条件：

1.1 Reagents: Potassium acetate Catalysts: [1,1′-Bis(diphenylphosphino)ferrocene]dichloropalladium Solvents: 1,4-Dioxane ; 80 °C

参考文献：

Fit-for-purpose synthesis of dual leucine zipper kinase (DLK) inhibitor GNE-834

Xu, Jie ; Carrera, Diane E.; Beaudry, Danial; Siu, Michael; Huestis, Malcolm P.; et al, Tetrahedron Letters, 2020, 61(43),

合成路线：1 步

_72%

反应条件：

1.1 Reagents: Potassium acetate Catalysts: Dichloro[1,1′-bis(diphenylphosphino)ferrocene]palladium(II) dichloromethane addu… Solvents: 1,2-Dimethoxyethane ; overnight, 80 °C; 80 °C → rt

参考文献：

Preparation of thiazolopyridinylacetamide derivatives and analogs for use as PI3K and mTOR kinase inhibitors

, World Intellectual Property Organization, , ,

合成路线：1 步

反应条件：

1.1 Reagents: Potassium acetate Catalysts: [1,1′-Bis(diphenylphosphino)ferrocene]dichloropalladium Solvents: 1,4-Dioxane ; overnight, 100 °C

参考文献：

Preparation of spiro compounds as Map4K1 inhibitors

, World Intellectual Property Organization, , ,

合成路线：1 步

反应条件：

1.1 Reagents: Potassium acetate Catalysts: [1,1′-Bis(diphenylphosphino)ferrocene]dichloropalladium Solvents: 1,4-Dioxane ; overnight, 115 °C; 115 °C → rt
1.2 Reagents: Water Solvents: Ethyl acetate

参考文献：

Preparation of 2-Morpholino-4,6-disubstituted pyrimidine analogues and their application as anticancer agents

, World Intellectual Property Organization, , ,

合成路线：1 步

反应条件：

1.1 Reagents: Potassium acetate Catalysts: Dichloro[1,1′-bis(diphenylphosphino)ferrocene]palladium(II) dichloromethane addu… Solvents: 1,4-Dioxane ; 5 h, 100 °C

参考文献：

Preparation of pyrazolopyridine compounds for the treatment of parasitic diseases

, World Intellectual Property Organization, , ,

合成路线：1 步

反应条件：

1.1 Reagents: Potassium acetate Catalysts: [1,1′-Bis(diphenylphosphino)ferrocene]dichloropalladium Solvents: Dimethylformamide ; 2 h, 150 °C

参考文献：

Structure guided optimization of a fragment hit to imidazopyridine inhibitors of PI3K

Pecchi, Sabina; Ni, Zhi-Jie; Han, Wooseok; Smith, Aaron; Lan, Jiong; et al, Bioorganic & Medicinal Chemistry Letters, 2013, 23(16), 4652-4656

合成路线：1 步

反应条件：

1.1 Reagents: Potassium acetate Solvents: 1,4-Dioxane ; rt
1.2 Catalysts: Dichloro[1,1′-bis(diphenylphosphino)ferrocene]palladium(II) dichloromethane addu… ; 8 h, 115 °C

参考文献：

1H-Imidazo[4,5-c]quinolinone compounds as protein kinase inhibitors and their preparation and use in the treatment of proliferative diseases

, World Intellectual Property Organization, , ,

合成路线：1 步

反应条件：

1.1 Reagents: Potassium acetate Catalysts: Dichloro[1,1′-bis(diphenylphosphino)ferrocene]palladium(II) dichloromethane addu… Solvents: 1,4-Dioxane ; 15 min, rt; 15 min, rt; 8 h, 115 °C

参考文献：

Preparation of substituted imidazopyridazine derivatives for use as PI3K lipid kinase inhibitors

, World Intellectual Property Organization, , ,

合成路线：1 步

反应条件：

1.1 Reagents: Potassium acetate Catalysts: Dichloro[1,1′-bis(diphenylphosphino)ferrocene]palladium(II) dichloromethane addu… Solvents: 1,4-Dioxane ; 8 h, 115 °C

参考文献：

Preparation of substituted imidazopyridazines and pyrrolopyrimidines as lipid kinase inhibitors

, World Intellectual Property Organization, , ,

合成路线：1 步

反应条件：

1.1 Reagents: Potassium acetate Catalysts: [1,1′-Bis(diphenylphosphino)ferrocene]dichloropalladium Solvents: Dimethylformamide ; 2 h, 150 °C; 150 °C → rt

参考文献：

Preparation of pyrazolo[3,4-d]pyrimidine derivatives for treating respiratory disorders

, World Intellectual Property Organization, , ,

合成路线：1 步

反应条件：

1.1 Reagents: Potassium acetate Catalysts: Dichloro[1,1′-bis(diphenylphosphino)ferrocene]palladium(II) dichloromethane addu… Solvents: 1,4-Dioxane ; 8 h, 115 °C

参考文献：

Preparation of 2,4-substituted quinazolines as lipid kinase inhibitors

, World Intellectual Property Organization, , ,

合成路线：1 步

反应条件：

1.1 Reagents: Potassium acetate Catalysts: [1,1′-Bis(diphenylphosphino)ferrocene]dichloropalladium Solvents: Dimethylformamide ; 2 h, 150 °C; 150 °C → rt

参考文献：

Preparation of imidazo[1,2-a]pyridines and imidazo[1,2-b]pyridazines as PI-3 kinase inhibitors

, World Intellectual Property Organization, , ,

合成路线：1 步