938043-30-2 (4-(4-甲基-1-哌嗪甲基)苯硼酸频哪酯,1-methyl-4-[[4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)phenyl]methyl]piperazine)

_100%

反应条件：

1.1 Reagents: 4-Methylmorpholine Solvents: Tetrahydrofuran ; 35 min, 150 °C
1.2 Reagents: Tris(hydroxymethyl)aminomethane , Methyl isocyanate Solvents: Tetrahydrofuran ; 5 min, 150 °C

参考文献：

Microwave-mediated synthesis of an arylboronate library

Spencer, John; Baltus, Christine B.; Patel, Hiren; Press, Neil J.; Callear, Samantha K.; et al, ACS Combinatorial Science, 2011, 13(1), 24-31

合成路线：1 步

_96%

反应条件：

1.1 4 h, 70 °C

参考文献：

Preparation of spiro-oxazolidinone compounds and their use as metabotropic glutamate receptor potentiators

, World Intellectual Property Organization, , ,

合成路线：1 步

_90%

反应条件：

1.1 Reagents: Potassium acetate Catalysts: [1,1′-Bis(diphenylphosphino)ferrocene]dichloropalladium Solvents: 1,4-Dioxane ; rt; 12 h, 110 °C

参考文献：

Preparation of peptidyl nitriles as dipeptidylpeptidase I inhibitors

, World Intellectual Property Organization, , ,

合成路线：1 步

302348-51-2

_83%

反应条件：

1.1 Catalysts: Sodium carbonate , Bis(dichloro(η6-p-cymene)ruthenium) , Bis[2-(diphenylphosphino)phenyl] ether Solvents: Xylene ; rt → 155 °C; 24 h, 155 °C

参考文献：

Synthesis of Amines with Pendant Boronic Esters by Borrowing Hydrogen Catalysis

Ma, Winson M. J.; James, Tony D.; Williams, Jonathan M. J., Organic Letters, 2013, 15(18), 4850-4853

合成路线：1 步

_82%

反应条件：

1.1 Reagents: Potassium acetate Catalysts: [1,1′-Bis(diphenylphosphino)ferrocene]dichloropalladium Solvents: 1,4-Dioxane ; 3 h, 110 °C

参考文献：

Preparation of novel 3-(substituted amino)-6-alkyl-pyrazine-2-carboxamide derivatives and uses thereof

, Korea, , ,

合成路线：1 步

_75%

反应条件：

1.1 Reagents: Triethylamine Solvents: Acetonitrile ; 3 h, rt
1.2 rt

参考文献：

Bis(het)aryl-1,2,3-triazole quinuclidines as α7 nicotinic acetylcholine receptor ligands: Synthesis, structure affinity relationships, agonism activity, [18F]-radiolabeling and PET study in rats

Ouach, Aziz; Vercouillie, Johnny; Bertrand, Emilie; Rodrigues, Nuno; Pin, Frederic; et al, European Journal of Medicinal Chemistry, 2019, 179, 449-469

合成路线：1 步

_75%

反应条件：

1.1 Reagents: Potassium acetate Catalysts: [1,1′-Bis(diphenylphosphino)ferrocene]dichloropalladium Solvents: 1,4-Dioxane ; 3 h, 110 °C

参考文献：

Preparation of peptidyl nitrile compounds as dipeptidyl peptidase I (DPPI) inhibitors

, World Intellectual Property Organization, , ,

合成路线：1 步

_60%

反应条件：

1.1 Reagents: Potassium carbonate Catalysts: Tetrakis(triphenylphosphine)palladium Solvents: 1,4-Dioxane ; overnight, reflux

参考文献：

Preparation of peptidyl nitrile compounds as dipeptidylpeptidase I inhibitors

, 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: 1,4-Dioxane ; 12 h, 80 °C

参考文献：

Preparation of pyrrolo[2,3-b]pyridines or pyrrolo[2,3-b]pyrazines as HPK1 inhibitor and the use thereof

, World Intellectual Property Organization, , ,

合成路线：1 步

_6%

反应条件：

1.1 Reagents: Potassium acetate Catalysts: Dichloro[1,1′-bis(diphenylphosphino)ferrocene]palladium(II) dichloromethane addu… Solvents: 1,4-Dioxane ; 2 h, 80 °C

参考文献：

Synthesis of fused heterocyclic PI3kα inhibitors treating cancers

, World Intellectual Property Organization, , ,

合成路线：1 步

反应条件：

1.1 Reagents: Potassium carbonate Solvents: Acetonitrile ; 4 h, rt

参考文献：

Structure-based design, synthesis, and evaluation of inhibitors with high selectivity for PARP-1 over PARP-2

Yu, Jiang; Luo, Lingling; Hu, Tong; Cui, Yating; Sun, Xiao; et al, European Journal of Medicinal Chemistry, 2022, 227,

合成路线：1 步

反应条件：

1.1 Reagents: Sodium carbonate Solvents: Acetone ; 1 h, rt

参考文献：

Preparation of pyridine-3-sulfonamide compounds as PI3-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 ; 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 Solvents: Tetrahydrofuran ; 2 - 12 h, reflux

参考文献：

Discovery of a novel class of triazolones as Checkpoint Kinase inhibitors-Hit to lead exploration

Oza, Vibha; Ashwell, Susan; Brassil, Patrick; Breed, Jason; Deng, Chun; et al, Bioorganic & Medicinal Chemistry Letters, 2010, 20(17), 5133-5138

合成路线：1 步

反应条件：

1.1 Reagents: Potassium carbonate Solvents: Dimethylformamide ; 45 min, rt → 80 °C

参考文献：

Heterocyclic compounds useful as MK2 inhibitors and their preparation, pharmaceutical compositions and use in the treatment of diseases

, World Intellectual Property Organization, , ,

合成路线：1 步

反应条件：

1.1 Reagents: Potassium carbonate Solvents: Dimethylformamide ; 20 h, rt

参考文献：

Preparation of bicyclic heterocyclic compounds as FGFR inhibitors

, World Intellectual Property Organization, , ,

合成路线：1 步

反应条件：

1.1 Solvents: Diethyl ether ; 14 h, rt

参考文献：

Preparation of tetrazolyl (or triazolyl) substituted pyridinamines or pyrimidinamines as c-Met protein kinase inhibitors

, World Intellectual Property Organization, , ,

合成路线：1 步

反应条件：

1.1 3 h, 70 - 75 °C; 75 °C → rt

参考文献：

Oxazolidinone compounds and their use as metabotropic glutamate receptor potentiators in the treatment of neurological and psychiatric disorders and preparation

, World Intellectual Property Organization, , ,

合成路线：1 步