943320-61-4 (3-炔基咪唑并[1,2-B]哒嗪,3-Ethynylimidazo[1,2-b]pyridazine)

_98%

反应条件：

1.1 Reagents: Potassium fluoride Solvents: Methanol , Water ; 20 min, rt

参考文献：

Preparation of piperazine derivative as Bcr-Abl inhibitor for treatment of cancer

, China, , ,

合成路线：1 步

_98%

反应条件：

1.1 Reagents: Potassium fluoride Solvents: Methanol , Water ; 20 min, rt

参考文献：

Bcr-abl diploid inhibitor, preparation method therefor, and uses thereof

, World Intellectual Property Organization, , ,

合成路线：1 步

_95%

反应条件：

1.1 Reagents: Tetrabutylammonium fluoride Solvents: Tetrahydrofuran ; 15 min, rt

参考文献：

Preparation of substituted tetrahydronaphthalene amide compound and its pharmaceutically acceptable salt useful in the treatment of cancer

, China, , ,

合成路线：1 步

_90%

反应条件：

1.1 Reagents: Potassium carbonate Solvents: Methanol ; 2 h, rt

参考文献：

Piperzine analogs useful for inhibiting RAF dimers and their preparation

, World Intellectual Property Organization, , ,

合成路线：1 步

_89%

反应条件：

1.1 Reagents: Potassium carbonate Solvents: Methanol ; 6 h, rt

参考文献：

Quinazoline compound and its application in preparation of antitumor drug

, China, , ,

合成路线：1 步

_89%

反应条件：

1.1 Reagents: Tetrabutylammonium fluoride Solvents: Tetrahydrofuran ; 15 min, rt

参考文献：

S-type or R-type tetrahydronaphthalene amide compounds, pharmaceutically acceptable salts thereof, preparation method and application thereof in preparation of antitumor drugs

, China, , ,

合成路线：1 步

_89%

反应条件：

1.1 Reagents: Potassium carbonate Solvents: Methanol ; 0.5 h, rt

参考文献：

Preparation of substituted benzamide compounds for treatment of tumor

, China, , ,

合成路线：1 步

_89%

反应条件：

1.1 Reagents: Lithium hydroxide Solvents: Tetrahydrofuran , Water ; 2 h, rt

参考文献：

Preparation of bicyclic alkyne derivatives as inhibitors of MAP kinase interacting kinases for therapy

, United Kingdom, , ,

合成路线：1 步

_89%

反应条件：

1.1 Reagents: Dicyclohexylamine , Triethylamine Catalysts: Cuprous iodide , Dichlorobis(triphenylphosphine)palladium ; 14 h, 80 °C
1.2 Catalysts: Tetrabutylammonium fluoride Solvents: Tetrahydrofuran ; 3 h, rt

参考文献：

Preparation of indan derivatives as protein kinase inhibitors

, China, , ,

合成路线：1 步

2445521-09-3

74-86-2

_82%

反应条件：

1.1 Reagents: Potassium carbonate Solvents: Dimethylformamide ; 3 h, 0.4 MPa, 20 - 25 °C

参考文献：

Preparation of Ponatinib intermediate 3-ethynylimidazo[1,2-b]pyridazine

, China, , ,

合成路线：1 步

_80%

反应条件：

1.1 Reagents: Potassium carbonate Solvents: Methanol ; 1 h, rt

参考文献：

Preparation of benzo[b][1,4]oxazepine derivative for the treatment of kinase-related disease

, Korea, , ,

合成路线：1 步

_80%

反应条件：

1.1 Reagents: Potassium carbonate Solvents: Methanol ; 1 h, rt

参考文献：

Aryl or heteroaryl derivative, and pharmaceutical composition comprising same as active ingredient for treatment of kinase-related disease

, World Intellectual Property Organization, , ,

合成路线：1 步

_80%

反应条件：

1.1 Reagents: Potassium carbonate Solvents: Methanol ; 1 h, rt

参考文献：

Preparation of N-(3-(imidazo[1,2-b]pyridazin-3-ylethynyl)-4-methylphenyl)-5-phenyl-4,5-dihydro-1H-pyrazole-1-carboxamide and related compound as kinase inhibitor

, World Intellectual Property Organization, , ,

合成路线：1 步

_80%

反应条件：

1.1 Reagents: Triethylamine Catalysts: Cuprous iodide , Dichlorobis(triphenylphosphine)palladium Solvents: Acetonitrile ; rt; 20 h, 100 °C
1.2 Reagents: Potassium carbonate Solvents: Methanol ; 0.5 h, rt

参考文献：

Design, Synthesis, and Biological Evaluation of 3-(1H-1,2,3-Triazol-1-yl)benzamide Derivatives as Potent Pan Bcr-Abl Inhibitors Including the Threonine315→Isoleucine315 Mutant

Li, Yupeng; Shen, Mengjie; Zhang, Zhang; Luo, Jinfeng; Pan, Xiaofen; et al, Journal of Medicinal Chemistry, 2012, 55(22), 10033-10046

合成路线：1 步

_75%

反应条件：

1.1 Reagents: Tetrabutylammonium fluoride Solvents: Tetrahydrofuran ; 30 min, rt

参考文献：

Aromatic acetylenyl benzamide compounds as protein kinase inhibitors and their preparation, pharmaceutical compositions and use in the treatment of diseases

, China, , ,

合成路线：1 步

_74%

反应条件：

1.1 Reagents: Triethylamine Catalysts: Triphenylphosphine , Cuprous iodide , Palladium, bis(acetonitrile)dichloro- Solvents: Acetonitrile ; overnight, rt → 80 °C
1.2 Reagents: Potassium carbonate Solvents: Methanol ; 1 h, 80 °C

参考文献：

Abelson non-tyrosine kinase compounds for the treatment of neurodegenerative diseases

, World Intellectual Property Organization, , ,

合成路线：1 步

_74%

反应条件：

1.1 Reagents: Triethylamine Catalysts: Triphenylphosphine , Cuprous iodide , Palladium, bis(acetonitrile)dichloro- Solvents: Acetonitrile ; overnight, 80 °C
1.2 Reagents: Potassium carbonate Solvents: Methanol ; 1 h, rt

参考文献：

Accelerated Discovery of Novel Ponatinib Analogs with Improved Properties for the Treatment of Parkinson's Disease

Kaiser, Thomas M. ; Dentmon, Zackery W. ; Dalloul, Christopher E.; Sharma, Savita K.; Liotta, Dennis C., ACS Medicinal Chemistry Letters, 2020, 11(4), 491-496

合成路线：1 步

_71%

反应条件：

1.1 Reagents: Diisopropylethylamine Catalysts: Cuprous iodide , Tetrakis(triphenylphosphine)palladium Solvents: Dimethylformamide ; 1 h, rt
1.2 Reagents: Tetrabutylammonium fluoride Solvents: Tetrahydrofuran ; 15 min, rt

参考文献：

Structure Guided Design of Potent and Selective Ponatinib-Based Hybrid Inhibitors for RIPK1

Najjar, Malek; Suebsuwong, Chalada; Ray, Soumya S.; Thapa, Roshan J.; Maki, Jenny L.; et al, Cell Reports, 2015, 10(11), 1850-1860

合成路线：1 步

_71%

反应条件：

1.1 Reagents: Tetrabutylammonium fluoride Solvents: Tetrahydrofuran ; 30 min, rt

参考文献：

Synthesis of antineoplastic agent Ponatinib

Xie, Ning; Li, Yan-yang; Zhao, Yan-jin; Li, Shu-xin, Zhongguo Xinyao Zazhi, 2013, 22(22), 2688-2691

合成路线：1 步

_69%