940284-98-0 (2-[4-(N-叔丁氧羰基)哌嗪-1-基]嘧啶-5-硼酸频哪醇酯,Tert-Butyl 4-(5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)pyrimidin-2-yl)piperazine-1-carboxylate)

_76%

反应条件：

1.1 Reagents: Potassium acetate Catalysts: (SP-4-3)-rel-(Methanesulfonato-κO)[2′-[(R)-methylamino-κN][1,1′-biphenyl]-2-yl-κ… Solvents: 2-Methyltetrahydrofuran ; 24 h, 90 °C

参考文献：

A Monophosphine Ligand Derived from Anthracene Photodimer: Synthetic Applications for Palladium-Catalyzed Coupling Reactions

Wang, Xin; Liu, Wei-Gang; Tung, Chen-Ho ; Wu, Li-Zhu ; Cong, Huan, Organic Letters, 2019, 21(20), 8158-8163

合成路线：1 步

1003845-08-6

57260-71-6

_72%

反应条件：

1.1 Reagents: Diisopropylethylamine Solvents: Ethanol ; 3 h, 80 °C

参考文献：

Heterobifunctional compounds for degradation of tropomyosin receptor kinase and their preparation

, World Intellectual Property Organization, , ,

合成路线：1 步

_63%

反应条件：

1.1 Reagents: Potassium carbonate Catalysts: Dichloro[1,1′-bis(diphenylphosphino)ferrocene]palladium(II) dichloromethane addu… Solvents: 1,4-Dioxane ; 17 h, 120 °C

参考文献：

Preparation of thiazolidine derivatives as Pim inhibitors

, World Intellectual Property Organization, , ,

合成路线：1 步

780705-64-8

_57%

反应条件：

1.1 Catalysts: 3,4,7,8-Tetramethyl-1,10-phenanthroline , Bis[(1,2,5,6-η)-1,5-cyclooctadiene]di-μ-methoxydiiridium Solvents: Tetrahydrofuran ; 1 h, 80 °C
1.2 Solvents: Tetrahydrofuran ; 30 h, rt

参考文献：

Iridium-Catalyzed C-H Borylation of Heteroarenes: Scope, Regioselectivity, Application to Late-Stage Functionalization, and Mechanism

Larsen, Matthew A.; Hartwig, John F., Journal of the American Chemical Society, 2014, 136(11), 4287-4299

合成路线：1 步

_55%

反应条件：

1.1 Reagents: Potassium acetate Catalysts: Palladium diacetate Solvents: Dimethylformamide ; rt → 85 °C; overnight, 85 °C

参考文献：

Preparation of substituted indole compound as 5-hydroxytryptamine reuptake inhibitor

, World Intellectual Property Organization, , ,

合成路线：1 步

_49%

反应条件：

1.1 Reagents: Potassium acetate Catalysts: [1,1′-Bis(diphenylphosphino)ferrocene]dichloropalladium Solvents: 1,4-Dioxane ; 3 h, 145 °C

参考文献：

Improvement of aqueous solubility of lapatinib-derived analogues: identification of a quinolinimine lead for human African trypanosomiasis drug development

Bachovchin, Kelly A.; Sharma, Amrita; Bag, Seema; Klug, Dana M.; Schneider, Katherine M.; et al, Journal of Medicinal Chemistry, 2019, 62(2), 665-687

合成路线：1 步

_44%

反应条件：

1.1 Reagents: Potassium acetate Solvents: 1,4-Dioxane ; 10 min, rt
1.2 Catalysts: Dichlorobis(triphenylphosphine)palladium ; overnight, 95 °C

参考文献：

Preparation of azaindoles as aurora kinase inhibitors for the treatment of cancer

, United States, , ,

合成路线：1 步

_33%

反应条件：

1.1 Reagents: Potassium acetate Catalysts: [1,1′-Bis(diphenylphosphino)ferrocene]dichloropalladium Solvents: 1,4-Dioxane ; 16 h, 90 °C

参考文献：

Preparation of substituted imidazo[1,2-a]pyridin-3-amines as autotaxin inhibitors

, United States, , ,

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 ; 2 h, 100 °C

参考文献：

Preparation of triazole-based compounds as nuclear export protein inhibitor

, China, , ,

合成路线：1 步

反应条件：

1.1 Reagents: Potassium acetate Catalysts: Palladium diacetate Solvents: Dimethylformamide ; 16 h, 70 °C

参考文献：

Preparation of substituted nitrogen containing heterocyclic derivatives useful as PCSK9 inhibitors for the treatment of hyperlipidemia

, World Intellectual Property Organization, , ,

合成路线：1 步

185990-03-8

反应条件：

1.1 Reagents: Potassium methoxide Solvents: Methyl ether ; 1 h, 30 °C

参考文献：

Boryl substitution of functionalized aryl-, heteroaryl- and alkenyl halides with silylborane and an alkoxy base: expanded scope and mechanistic studies

Yamamoto, Eiji; Ukigai, Satoshi; Ito, Hajime, Chemical Science, 2015, 6(5), 2943-2951

合成路线：1 步

反应条件：

1.1 Reagents: Potassium acetate Catalysts: [1,1′-Bis(diphenylphosphino)ferrocene]dichloropalladium Solvents: Dimethyl sulfoxide ; overnight, 120 °C

参考文献：

Preparation of heterocyclic compounds as CCR4 or TARC and/or MDC function regulators

, Japan, , ,

合成路线：1 步

反应条件：

1.1 Reagents: Potassium carbonate Solvents: Acetonitrile ; 25 °C; 6 h, 100 °C; 100 °C → 25 °C
1.2 Reagents: Potassium acetate Catalysts: [1,1′-Bis(diphenylphosphino)ferrocene]dichloropalladium Solvents: 1,4-Dioxane ; 25 °C; 6 h, 80 - 90 °C; 90 °C → 25 °C

参考文献：

Preparation of benzothiazoles and aza-analogues as antibacterial agents

, World Intellectual Property Organization, , ,

合成路线：1 步

反应条件：

1.1 Reagents: Potassium acetate Catalysts: Tricyclohexylphosphine , Tris(dibenzylideneacetone)dipalladium Solvents: 1,4-Dioxane ; 5 h, rt → 100 °C

参考文献：

Preparation of condensed thiazoles as antibacterial agents

, 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: Dimethyl sulfoxide ; 4 h, 80 °C; overnight, 100 °C

参考文献：

Preparation of pyrazolopyrimidine derivatives or analogs thereof as CCR4 function modulators

, Japan, , ,

合成路线：1 步

参考文献：

Preparation of substituted pyrazolo[1,5-a]pyridines as inhibitors of FGFR tyrosine kinases for the treatment of FGFRs-mediated diseases

, World Intellectual Property Organization, , ,

合成路线：1 步