937046-95-2 ((1H-吡咯-1-基)氨基甲酸叔丁酯,N-(1H-pyrrol-1-yl)(tert-butoxy)formamide)

_94%

反应条件：

1.1 Catalysts: Squaraine Solvents: 1,4-Dioxane ; rt; rt → 90 °C; 3 h, pH 6.0, 90 °C; 90 °C → 98 °C; 4 h, 98 °C; 98 °C → rt
1.2 Reagents: Sodium carbonate Solvents: Water ; 10 min, rt

参考文献：

Green preparation of remdesivir intermediate 7-iodopyrrolo[2,1-F][1,2,4]triazine-4-amine

, China, , ,

合成路线：1 步

_89%

反应条件：

1.1 Reagents: Hydrochloric acid Solvents: N-Methyl-2-pyrrolidone , Water ; 33 h, 90 °C

参考文献：

Preparation of substituted bicyclic heteroaryls as CRTH2 antagonists

, World Intellectual Property Organization, , ,

合成路线：1 步

_86%

反应条件：

1.1 Reagents: Hydrochloric acid Solvents: N-Methyl-2-pyrrolidone , Water ; rt; 20 h, rt → 70 °C

参考文献：

Method for preparing 6-bromo-3H-pyrrolo[2,1-f][1,2,4]triazin-4-one by esterification

, China, , ,

合成路线：1 步

_77%

参考文献：

Facile and Scalable Methodology for the Pyrrolo[2,1-f][1,2,4]triazine of Remdesivir

Roy, Sarabindu; Yadaw, Ajay; Roy, Subho; Sirasani, Gopal; Gangu, Aravind; et al, Organic Process Research & Development, 2022, 26(1), 82-90

合成路线：1 步

109-99-9

_71%

反应条件：

1.1 Reagents: Hydrochloric acid Solvents: N-Methyl-2-pyrrolidone , Water ; rt; rt → 90 °C; 12 h, 90 °C

参考文献：

Synthesis of 7-bromopyrrolo[2,1-f][1,2,4]triazin-4-amine

Zheng, Jun; Cao, Guo-rui, Huaxue Shiji, 2020, 42(5), 608-611

合成路线：1 步

_70%

反应条件：

1.1 Reagents: Hydrochloric acid Solvents: 1,4-Dioxane , Water ; rt; 10 h, rt → 90 °C

参考文献：

Method for preparing 7-bromopyrrolo[2,1-f][1,2,4]triazin-4-amine as GS-441524 intermediate for treating feline infectious peritonitis (FIP)

, China, , ,

合成路线：1 步

_68%

反应条件：

1.1 Reagents: Hydrochloric acid Solvents: 1,4-Dioxane , Water ; overnight, rt → 90 °C

参考文献：

N-heterocycle-containing derivative and its pharmaceutical application

, China, , ,

合成路线：1 步

_60%

反应条件：

1.1 Reagents: Pyridine , Pyridinium chloride Solvents: 1,4-Dioxane ; 7 h, 102 °C

参考文献：

Preparation of the monohydrate of rogaratinib hydrochloride and solid states thereof

, World Intellectual Property Organization, , ,

合成路线：1 步

24424-99-5

765-39-9

_59%

反应条件：

1.1 Reagents: Potassium tert-butoxide Solvents: Dimethylformamide ; 5 h, 85 °C

参考文献：

Dibromides of BOC-protected 1-aminopyrrole and 4-amino-1,2,4-triazole: synthesis, X-ray molecular structure, and NMR behavior

Yamamoto, Takakazu; Tanaka, Gentaro; Fukumoto, Hiroki; Koizumi, Take-aki, Heterocycles, 2009, 78(1), 117-125

合成路线：1 步

_59%

反应条件：

1.1 Reagents: Hydrochloric acid Solvents: 1,4-Dioxane ; > 1 h, 90 °C
1.2 Reagents: Sodium bicarbonate Solvents: Water ; neutralized, cooled

参考文献：

Preparation of substituted 4-amino-pyrrolotriazine derivatives useful for treating hyper-proliferative disorders and diseases associated with angiogenesis

, World Intellectual Property Organization, , ,

合成路线：1 步

_59%

反应条件：

1.1 Reagents: Hydrochloric acid Solvents: 1,4-Dioxane , Water ; > 1 h, 90 °C; cooled
1.2 Reagents: Sodium bicarbonate Solvents: Water ; neutralized

参考文献：

Preparation of pyrrolo[2,1-f][1,2,4]triazin-4-ylamines as IGF-1R kinase inhibitors for the treatment of cancer and other hyperproliferative diseases

, World Intellectual Property Organization, , ,

合成路线：1 步

_58%

反应条件：

1.1 Reagents: Hydrochloric acid Solvents: 1,4-Dioxane , Water ; rt; 48 h, rt → 100 °C

参考文献：

Preparing method and application of tricyclic compounds capable of inhibiting EGFR kinase mutant

, China, , ,

合成路线：1 步

_57%

反应条件：

1.1 Reagents: Hydrochloric acid Solvents: 1,4-Dioxane ; 20 h, 90 °C; 90 °C → 20 °C
1.2 Reagents: Sodium bicarbonate Solvents: Water ; neutralized, rt

参考文献：

Preparation of multicyclic heterocycles as Janus kinase inhibitors for treating cancer or modifying an immune response

, World Intellectual Property Organization, , ,

合成路线：1 步

_57%

反应条件：

1.1 Reagents: Hydrochloric acid Solvents: 1,4-Dioxane , Water ; 20 h, 90 °C; 90 °C → 20 °C
1.2 Reagents: Sodium bicarbonate Solvents: Water ; neutralized

参考文献：

Pyrrolopyridazines and pyrrolotriazines as janus kinase inhibitors and their preparation and use for the treatment of JAK-associated diseases

, World Intellectual Property Organization, , ,

合成路线：1 步

_57%

反应条件：

1.1 Reagents: Sodium hydroxide Solvents: 1,4-Dioxane , Water ; 20 h, 90 °C; 90 °C → 20 °C
1.2 Reagents: Sodium bicarbonate Solvents: Water ; neutralized

参考文献：

Preparation of piperidine derivatives as immunosuppressant for the treatment of diseases associated with pathologic JAK3 activation

, World Intellectual Property Organization, , ,

合成路线：1 步

_50%

反应条件：

1.1 Reagents: Hydrochloric acid Solvents: N-Methyl-2-pyrrolidone , Water ; rt → 90 °C; 1 h, 90 °C; 12 h, 90 °C; 90 °C → 24 °C
1.2 Solvents: Water ; 25 min, 24 °C

参考文献：

Discovery and Process Synthesis of Novel 2,7-Pyrrolo[2,1-f][1,2,4]triazines

Thieu, Tho; Sclafani, Joseph A.; Levy, Daniel V.; McLean, Andrew; Breslin, Henry J.; et al, Organic Letters, 2011, 13(16), 4204-4207

合成路线：1 步

_41%

反应条件：

1.1 Catalysts: Hydrochloric acid Solvents: 1,4-Dioxane ; 90 °C

参考文献：

Discovery of Rogaratinib (BAY 1163877): a pan-FGFR Inhibitor

Collin, Marie-Pierre ; Lobell, Mario; Huebsch, Walter; Brohm, Dirk; Schirok, Hartmut; et al, ChemMedChem, 2018, 13(5), 437-445

合成路线：1 步

_40%

反应条件：

1.1 Reagents: Hydrochloric acid Solvents: 1,4-Dioxane ; > 1 h, 90 °C
1.2 Reagents: Sodium bicarbonate Solvents: Water
1.3 Reagents: Hydrochloric acid Solvents: Water ; neutralized

参考文献：

Preparation of substituted 4-aminopyrrolotriazine derivatives useful for treating hyperproliferative disorders and diseases associated with angiogenesis

, World Intellectual Property Organization, , ,

合成路线：1 步