923036-30-0 (N-甲基-N-((3R,4R)-4-甲基-1-苄基-3-哌啶基)-7-((4-甲基苯基)磺酰基)7H,N-[(3R,4R)-1-benzyl-4-methyl-3-piperidyl]-N-methyl-7-(p-tolylsulfonyl)pyrrolo[2,3-d]pyrimidin-4-amine)

906092-45-3

_94%

反应条件：

1.1 Reagents: Sodium carbonate ; rt; rt → 95 °C
1.2 2 h, 95 °C

参考文献：

Process for the preparation of tofacitinib citrate intermediate N-methyl-N-[(3R,4R)-4-methyl-1-(phenylmethyl)-3-piperidinyl]-7-[(4-methylphenyl)sulfonyl]-7H-pyrrolo[2,3-d]pyrimidin-4-amine

, China, , ,

合成路线：1 步

_93%

反应条件：

1.1 Reagents: Diisopropylethylamine Solvents: Dimethyl sulfoxide , Water ; 9 h, rt → 107 °C

参考文献：

Industrialized production of Tofacitinib citrate

, China, , ,

合成路线：1 步

_90%

反应条件：

1.1 Reagents: Potassium carbonate Solvents: Water ; 16 h, 100 °C

参考文献：

Isoxazole derivative that inhibits activity of janus kinases (jaks)

, World Intellectual Property Organization, , ,

合成路线：1 步

_89%

反应条件：

1.1 Reagents: Potassium carbonate Solvents: Water ; 90 °C

参考文献：

An Improved and Efficient Process for the Preparation of Tofacitinib Citrate

Patil, Yogesh S.; Bonde, Nilesh L.; Kekan, Ankush S.; Sathe, Dhananjay G.; Das, Arijit, Organic Process Research & Development, 2014, 18(12), 1714-1720

合成路线：1 步

_88%

反应条件：

1.1 Reagents: Potassium carbonate Solvents: Water ; 16 h, reflux

参考文献：

Synthesis and evaluation of tofacitinib analogs designed to mitigate metabolic activation

Tateishi, Yasuhiro ; Shibazaki, Chikako; Takahashi, Kyoko ; Nakamura, Shigeo ; Kazuki, Yasuhiro; et al, Drug Metabolism and Pharmacokinetics, 2022, 43,

合成路线：1 步

_87%

反应条件：

1.1 Reagents: Potassium carbonate Solvents: Water ; 16 h, reflux; reflux → rt

参考文献：

Examining the chirality, conformation and selective kinase inhibition of 3-((3R,4R)-4-methyl-3-(methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)piperidin-1-yl)-3-oxopropanenitrile (CP-690,550)

Jiang, Jian-kang; Ghoreschi, Kamran; Deflorian, Francesca; Chen, Zhi; Perreira, Melissa; et al, Journal of Medicinal Chemistry, 2008, 51(24), 8012-8018

合成路线：1 步

_86%

反应条件：

1.1 Reagents: Potassium carbonate Solvents: Tetrahydrofuran , Water ; 8 - 10 h, reflux

参考文献：

Preparation method of tofacitinib as JAK inhibitor with high yield

, China, , ,

合成路线：1 步

_82%

反应条件：

1.1 Reagents: Potassium carbonate Solvents: Water ; 10 h, rt → 105 °C

参考文献：

Process for preparation of piperidinylaminopyrrolopyrimidines from activated pyrrolopyrimidines and piperidinylamines.

, World Intellectual Property Organization, , ,

合成路线：1 步

_77%

反应条件：

1.1 Reagents: Diisopropylethylamine Solvents: 1,4-Dioxane ; 4 h, rt → reflux

参考文献：

Preparation of tofacitinib intermediate

, China, , ,

合成路线：1 步

_75%

反应条件：

1.1 Reagents: Potassium carbonate Solvents: Methanol ; rt → 65 °C; 8 h, 60 - 65 °C

参考文献：

Process for the preparation of tofacitinib citrate

, China, , ,

合成路线：1 步

2250243-22-0

_74%

反应条件：

1.1 Reagents: Sodium carbonate Solvents: Dimethylformamide ; 10 h, rt

参考文献：

Method for preparing N-methyl-N-(4-methylpiperidin)-3-yl-7H-pyrrolopyrimidin-4-amine

, China, , ,

合成路线：1 步

_69%

反应条件：

1.1 Reagents: Potassium carbonate Solvents: Water ; 18 h, 105 °C

参考文献：

Preparation of heteroaromatic compounds for treating autoimmune or proliferative diseases

, China, , ,

合成路线：1 步

反应条件：

1.1 Reagents: Potassium carbonate Solvents: Water ; rt → 95 °C; 12 h, 95 °C; 95 °C → rt; 4 h, rt

参考文献：

A process for the preparation of 1-benzyl-N,4-dimethylpiperidin-3-amine, an useful intermediate for preparation of tofacitinib

, India, , ,

合成路线：1 步

反应条件：

1.1 Reagents: Potassium carbonate Solvents: Water ; 100 °C

参考文献：

Preparation of tofacitinib citrate

, China, , ,

合成路线：1 步