Molecular Formula | C6H6ClNOS |
Molar Mass | 175.64 |
Melting Point | 164-166°C |
Solubility | Chloroform (Slightly), Methanol (Slightly) |
Appearance | Solid |
Color | White to Off-White |
Storage Condition | Refrigerator |
Use | 5-chlorothiophene-2-formylamine is an impurity D in the synthesis of rivaroxaban. Rivaroxaban is an anticoagulant, an oral drug that is highly selective and directly inhibits factor Xa, inhibiting thrombin production and thrombosis. |
preparation | step ① adding 5-chlorothiophene -2-formic acid and dichloromethane to reaction vessel d, adding dichlorosulfoxide dropwise at 0 ℃, stirring at room temperature for 4 hours after the dropwise addition; After step ②, add an aqueous solution with a mass concentration of 40% methylamine dropwise at 0 ℃, complete the dropwise addition, and stir at room temperature for 18 hours; after step (3), the filter cake is dried to constant weight by blowing at 55 ℃, and the solid is 5-chlorothiophene-2-formylmethylamine. The addition amount of the aqueous solution of 5-chlorothiophene-2-formic acid, dichloromethane, dichlorosulfoxide and 40% methylamine is 20g,500ml,49.52g and 107.73g;5-chlorothiophene-2-formylmethylamine is 10g, the yield is 41.03%, and the purity is 99.80%. |