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Purity:99%
The invention relates to synthesis of ba...
The present disclosure provides a Barici...
Nine compounds potentially related to th...
Method and intermediates are disclosed f...
4-chloro-7-azaindole
(4-{1-[3-(cyanomethyl)-1-(ethylsulphonyl)azetidin-3-yl]-1H-pyrazol-4-yl}-7H-pyrrolo[2,3-d]pyrimidin-7-yl)methyl 2,2-dimethylpropanoate
| Conditions | Yield |
|---|---|
|
Multi-step reaction with 4 steps
1: potassium carbonate / N,N-dimethyl-formamide / 16 h / 20 °C
2: bis-triphenylphosphine-palladium(II) chloride; potassium carbonate / 1,4-dioxane; water / 3 h / 72 °C / Inert atmosphere
3: acetyl chloride / methanol / 6 h / 5 - 20 °C
4: 1,8-diazabicyclo[5.4.0]undec-7-ene / N,N-dimethyl-formamide / 3 h / 5 - 10 °C
With
bis-triphenylphosphine-palladium(II) chloride; potassium carbonate; 1,8-diazabicyclo[5.4.0]undec-7-ene; acetyl chloride;
In
1,4-dioxane; methanol; water; N,N-dimethyl-formamide;
|
|
|
Multi-step reaction with 4 steps
1: potassium carbonate / N,N-dimethyl-formamide / 16 h / 20 °C
2: bis(1,5-cyclooctadiene)nickel (0); tricyclohexylphosphine; potassium carbonate / water; tert-butyl alcohol / 3 h / 40 °C / Glovebox
3: hydrogenchloride / water; tetrahydrofuran / 6 h / 5 - 20 °C
4: 1,8-diazabicyclo[5.4.0]undec-7-ene / N,N-dimethyl-formamide / 3 h / 5 - 10 °C
With
hydrogenchloride; bis(1,5-cyclooctadiene)nickel (0); potassium carbonate; 1,8-diazabicyclo[5.4.0]undec-7-ene; tricyclohexylphosphine;
In
tetrahydrofuran; water; N,N-dimethyl-formamide; tert-butyl alcohol;
|
(4-{1-[3-(cyanomethyl)azetidin-3-yl]-1H-pyrazol-4-yl}-7H-pyrrolo[2,3-d]pyrimidin-7-yl)methyl 2,2-dimethylpropanoate
(4-{1-[3-(cyanomethyl)-1-(ethylsulphonyl)azetidin-3-yl]-1H-pyrazol-4-yl}-7H-pyrrolo[2,3-d]pyrimidin-7-yl)methyl 2,2-dimethylpropanoate
| Conditions | Yield |
|---|---|
|
With
N-ethyl-N,N-diisopropylamine; Ethanesulfonyl chloride;
In
ethyl acetate;
at 0 - 20 ℃;
for 1.5h;
Solvent;
Temperature;
|
95.7% |
[4-(1H-pyrazol-4-yl)-7H-pyrrolo[2,3-d]pyrimidin-7-yl]methyl 2,2-dimethylpropanoate
2-[1-(ethanesulfonyl)azetidin-3-ylidene]acetonitrile
3-(cyanomethylene)azetidine-1-carboxylic acid tert-butyl ester
[4-[1-(1-ethoxyethyl)-1H-pyrazol-4-yl]-7H-pyrrolo[2,3-d]pyrimidin-7-yl]methyl pivalate
Baricitinib
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