937046-96-3 ((2-氰基-1H-吡咯-1-基)氨基甲酸叔丁酯,N-(2-cyano-1H-pyrrol-1-yl)(tert-butoxy)formamide)

_96%

反应条件：

1.1 Solvents: Dimethylformamide , Acetonitrile ; 0 °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

_95%

反应条件：

1.1 Solvents: Acetonitrile ; 0 °C; 1 h, 0 °C
1.2 Solvents: Dimethylformamide ; 1 h, 0 °C
1.3 Reagents: Water ; cooled
1.4 Reagents: Sodium carbonate Solvents: Water ; neutralized

参考文献：

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

, China, , ,

合成路线：1 步

75-12-7

_93%

反应条件：

1.1 Reagents: Chlorosulfonyl isocyanate Solvents: Acetonitrile ; 0 °C; 1 h, -5 °C
1.2 1 h, -5 °C; 2 h, -5 °C
1.3 Reagents: Water ; 1 h, -5 °C; 2 h, 0.09 MPa, 30 °C

参考文献：

Green preparation of remdesivir intermediate

, China, , ,

合成路线：1 步

_87%

反应条件：

1.1 Solvents: Acetonitrile ; 0 °C; 20 min, < 5 °C
1.2 Reagents: Dimethylformamide ; 30 min, < 5 °C; 30 min, 0 °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

_83%

反应条件：

1.1 Solvents: Acetonitrile ; 1 h, 0 °C
1.2 Solvents: Dimethylformamide ; 1 h, 0 °C; 0 °C → rt
1.3 Reagents: Water ; 0 °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

_80%

反应条件：

1.1 Solvents: Dimethylformamide ; 2.5 h, 0 °C; 1 h, 0 °C
1.2 Reagents: Ammonium bicarbonate Solvents: Water ; < 25 °C
1.3 Solvents: Dimethylformamide , Water ; 2 h, 22 °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

_77%

反应条件：

1.1 Solvents: Acetonitrile ; rt → 0 °C; < 5 °C; 20 min, < 5 °C; 45 min, < 5 °C
1.2 Reagents: Dimethylformamide ; < 5 °C; 45 min, 0 °C; 0 °C → rt
1.3 Reagents: Water ; 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

75-05-8

_77%

反应条件：

1.1 Reagents: Chlorosulfonyl isocyanate Solvents: Acetonitrile ; rt → 0 °C; 20 min, < 5 °C; 45 min, < 5 °C
1.2 Reagents: Dimethylformamide ; 45 min, < 5 °C; 5 °C → rt

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

_77%

反应条件：

1.1 Solvents: Acetonitrile ; rt → 0 °C; < 5 °C; 45 min, < 5 °C
1.2 Reagents: Dimethylformamide ; < 5 °C; 45 min, 0 °C; 0 °C → rt

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

_66%

反应条件：

1.1 Solvents: Acetonitrile ; 30 min, 0 °C
1.2 Solvents: Dimethylformamide ; < 5 °C; 1 h, 0 °C

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

_66%

反应条件：

1.1 Solvents: Acetonitrile ; 0 °C; 30 min, 0 °C
1.2 Solvents: Dimethylformamide ; 1 h, 0 °C

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

_66%

反应条件：

1.1 Solvents: Acetonitrile ; 30 min, 0 °C
1.2 Solvents: Dimethylformamide ; < 5 °C; 1 h, 0 °C

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

_62%

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

_54%

反应条件：

1.1 Solvents: Acetonitrile ; 0 °C; 1 h, 0 °C
1.2 Solvents: Dimethylformamide ; 0 °C; 1 h, 0 °C
1.3 Reagents: Water

参考文献：

N-heterocycle-containing derivative and its pharmaceutical application

, China, , ,

合成路线：1 步

反应条件：

1.1 Solvents: Dimethylformamide , Acetonitrile ; < 5 °C; 45 min, < 5 °C; 30 min, < 5 °C
1.2 Reagents: Water ; cooled
1.3 Reagents: Sodium carbonate Solvents: Water

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

反应条件：

1.1 Solvents: Acetonitrile ; 1 h, rt
1.2 Solvents: Dimethylformamide ; 1 h, rt

参考文献：

Preparation of CDK kinase inhibitors

, World Intellectual Property Organization, , ,

合成路线：1 步

反应条件：

1.1 Solvents: Acetonitrile ; 0 °C; 30 min, 0 °C; 45 min, 0 °C
1.2 Solvents: Dimethylformamide ; 45 min, 0 °C; 0 °C → 25 °C

参考文献：

FGFR inhibitor and medical application thereof

, World Intellectual Property Organization, , ,

合成路线：1 步

反应条件：

1.1 Solvents: Acetonitrile ; -7 °C; 1 h, 0 °C
1.2 Reagents: Dimethylformamide ; 1 h, 5 °C

参考文献：

Preparation of pyrrolotriazine derivatives as Btk inhibitors

, World Intellectual Property Organization, , ,

合成路线：1 步