4-ХЛОРО-7-ТОСИЛ-7H-ПИРРОЛО [2,3-D] ПИРИМИДИН
4-ХЛОРО-7-ТОСИЛ-7H-ПИРРОЛО [2,3-D] ПИРИМИДИН атрибут
| Температура плавления: |
145.0 to 149.0 °C |
| Температура кипения: |
505.3±60.0 °C(Predicted) |
| плотность: |
1.49 |
| температура хранения: |
Keep in dark place,Sealed in dry,Room Temperature |
| растворимость: |
Chloroform (Slightly), DMSO (Slightly) |
| форма: |
порошок до кристалла |
| пка: |
1.73±0.30(Predicted) |
| цвет: |
White to Orange to Green |
| InChI: |
InChI=1S/C13H10ClN3O2S/c1-9-2-4-10(5-3-9)20(18,19)17-7-6-11-12(14)15-8-16-13(11)17/h2-8H,1H3 |
| ИнЧИКей: |
BTOJSYRZQZOMOK-UHFFFAOYSA-N |
| SMILES: |
C1=NC(Cl)=C2C=CN(S(C3=CC=C(C)C=C3)(=O)=O)C2=N1 |
4-ХЛОРО-7-ТОСИЛ-7H-ПИРРОЛО [2,3-D] ПИРИМИДИН химические свойства, назначение, производство
Использование
4-Chloro-7-tosyl-7H-pyrrolo[2,3-d]pyrimidine is a reagent in the synthesis of (+)-tofacitinib, a selective Janus kinase 3 inhibitor (JAK3) and an immunosuppressant drug.
Синтез
4-Chloro-7H-pyrrolo[2,3-d]pyrimidine (2kg, 12.96mol) and dichloromethane (40L) were added to the reaction flask at room temperature, stirred and dissolved. Triethylamine (3.88 kg, 38.4 mol) and 4-dimethylamino pyridine (157.6 g, 1.28 mol) were added in that order, and after stirring and dissolved, p-toluenesulfonyl chloride (2.6 kg, 13.6 mol) was added dropwise at 0 °C. The chloromethane (30 L) solution was added dropwise, and the mixture was stirred at room temperature for 30 min. After the TLC was applied, the mixture was washed with water (16L×3). 4-Chloro-7-tosyl-7H-pyrrolo[2,3-d]pyrimidine (3.9 kg, yield 97.7%) was obtained after drying under reduced pressure.
![4-Chloro-7-tosyl-7H-pyrrolo[2,3-d]pyrimidine](/NewsImg/2024-04-11/6384842224037577876641123.png "4-Chloro-7-tosyl-7H-pyrrolo[2,3-d]pyrimidine")
4-ХЛОРО-7-ТОСИЛ-7H-ПИРРОЛО [2,3-D] ПИРИМИДИН препаратная продукция и сырье
сырьё
препарат
4-ХЛОРО-7-ТОСИЛ-7H-ПИРРОЛО [2,3-D] ПИРИМИДИН поставщик
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