edoxaban Raw Materials powder edoxaban

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edoxaban powder Usage and Synthesis.

Edoxaban is used in a wide range of applications, including ‌ to reduce the risk of stroke and systemic embolism in patients with non-valvular atrial fibrillation (‌NVAF) ‌, ‌ and as a treatment for deep vein thrombosis (‌DVT) ‌ and pulmonary embolism (‌PE) ‌. ‌ ‌ it is also used for hip replacement, ‌ knee replacement and after hip fracture surgery, ‌ for the prevention of venous thromboembolism. ‌ These uses of Edoxaban are based on its ability to effectively inhibit FXa, ‌ reduce thrombus formation, and ‌ to protect patients from thrombosis related complications. ‌

Uses of edoxaban powder.

Edoxaban has anticoagulant effects and is mainly used for stroke prevention in patients with non-valvular atrial fibrillation and for the prevention of venous thromboembolism after hip and knee replacement and hip fracture surgery. Edoxaban is the fourth new oral anticoagulant approved by the US FDA after Dabigatrun, Rivaroxaban and Apixaban. In the process of using edoxaban, we should also pay attention to its adverse reactions, which may induce stroke and may also occur epidural hematoma. If there is renal insufficiency, such as creatinine clearance less than 95ml/min, do not use the drug.

Pharmacological action of edoxaban powder.

Class according to the degree of sand is a reversible factor Xa inhibitors, highly selective, can inhibit FXa directly, the result can prolong prothrombin time (prothrombintime, PT) and activated partial coagulation time (activatedpartialthromboplastintime, APTT) live enzymes, Ultimately, thrombosis is inhibited. Due to the amplification of biological signals in the clotting process, one Factor Xa inhibitor molecule can inhibit the physiological effects of 138 prothrombin molecules, so Factor Xa inhibitors are more effective than thrombin inhibitors. Therapeutic dose class of PT, international standardization in accordance with the degree of sand ratio (internationalnormalizedratio, INR) and APTT is influential, but changes smaller; Peak concentration (Cmax) can be reached 1 to 2 hours after oral administration.

Preparation method of Bulk edoxaban powder.

Methyl sulfonic acid (66ml) was added to a acetonitrile (1900ml) suspension of N-(5-clopiperidin-2-yl)-N'-[(1S,2R,4S)-4-(N, n-dimethylformylamino)-2-(aminotert-butoxycarbonyl) cyclohexyl] oxamide (95.1g) at room temperature and stirred at this temperature for 2 h. Under cold conditions, triethylamine (155ml),4,5,6, 7-tetrahydro-5-methyl-thiazolium [5, 4-C] pyridine-2-carboxylate hydrochloride (52.5g), 1-hydroxybenzotriazole (33.0g), 1-ethyl -(3-dimethylaminopropyl) carbodiimide hydrochloride (46.8g) were added to the reaction solution. Stir at room temperature for 16 hours. Add triethylamine and water, stir under cold for 1 hour, filter and crystallize to obtain compound (1), i.e. Edoxaban 103.2g.

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