918524-63-7 (2-甲基哌嗪-5-吡啶硼酸频哪醇酯,1-Methyl-4-(5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)pyridin-2-yl)piperazine)

_75%

反应条件：

1.1 Reagents: Potassium acetate Catalysts: [1,1′-Bis(diphenylphosphino)ferrocene]dichloropalladium Solvents: Dimethylformamide , 1,4-Dioxane ; overnight, 95 °C

参考文献：

Sulfonyl-substituted benzoheterocyclic derivative as EZH2 inhibitor and its preparation

, World Intellectual Property Organization, , ,

合成路线：1 步

_56%

反应条件：

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

参考文献：

EZH2 inhibitors and uses thereof

, World Intellectual Property Organization, , ,

合成路线：1 步

61676-62-8

_45%

反应条件：

1.1 Reagents: Butyllithium Solvents: Tetrahydrofuran , Hexane ; -78 °C; 30 min, -78 °C
1.2 -78 °C; -78 °C → rt; 22 h, rt

参考文献：

Preparation of thiazolidine derivatives as Pim inhibitors

, World Intellectual Property Organization, , ,

合成路线：1 步

_28%

反应条件：

1.1 Reagents: Potassium acetate Catalysts: [1,1′-Bis(diphenylphosphino)ferrocene]dichloropalladium Solvents: Dimethylformamide ; overnight, rt → 80 °C

参考文献：

Preparation of heterocycles as antitumor agents

, China, , ,

合成路线：1 步

_14%

反应条件：

1.1 Reagents: Potassium acetate Catalysts: Dichloro[1,1′-bis(diphenylphosphino)ferrocene]palladium(II) dichloromethane addu… Solvents: 1,4-Dioxane ; 3 h, rt → 80 °C; cooled

参考文献：

Preparation of 1,4-benzodiazepinone compounds and their use in treating cancer

, 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 ; overnight, 80 °C

参考文献：

Process for preparation of 1,5,7-tri-substituted isoquinoline derivatives and use in medicines

, 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 ; 12 h, 90 °C

参考文献：

Preparation of pyridonaphthyridine derivatives as PI3K and mTOR inhibitors

, World Intellectual Property Organization, , ,

合成路线：1 步

61676-62-8

反应条件：

1.1 Reagents: Butyllithium Solvents: Tetrahydrofuran , Hexane ; -78 °C; 30 min, -78 °C
1.2 2 h, -78 °C; -78 °C → rt
1.3 Reagents: Ammonium chloride Solvents: Water ; rt

参考文献：

Pyrrole derivatives useful for the treatment of cytokine-mediated diseases and their preparation

, World Intellectual Property Organization, , ,

合成路线：1 步

61676-62-8

反应条件：

1.1 Reagents: Butyllithium Solvents: Tetrahydrofuran , Hexane ; rt → -78 °C; -78 °C; 30 min, -78 °C
1.2 2 h, -78 °C; -78 °C → rt
1.3 Reagents: Sodium bicarbonate Solvents: Water

参考文献：

Preparation of bicyclic aromatic compounds as inhibitors of mitogen-activated protein kinase-activated protein kinase-2

, World Intellectual Property Organization, , ,

合成路线：1 步

参考文献：

The Discovery of PLK4 Inhibitors: (E)-3-((1H-Indazol-6-yl)methylene)indolin-2-ones as Novel Antiproliferative Agents

Laufer, Radoslaw; Forrest, Bryan; Li, Sze-Wan; Liu, Yong; Sampson, Peter; et al, Journal of Medicinal Chemistry, 2013, 56(15), 6069-6087

合成路线：1 步