| 摘要 |
<p>This invention refers to the preparation of a direct thrombin inhibitor, especially the application of a thrombin inhibitor of 21 (s) Argatroban. The chemical name of 21(S) Argatroban is: (2R, 4R) -1- { (2S) -5- [ ( Aminoiminomethyl) amino] -1-oxo-2-{ [ (3S) -1, 2, 3, 4-tetrahydro-3-methyl-8- quinolinyl] sulf onyl] amino] pentyl] -4-methyl-2-piperidine carboxylic acid, and the supplies which can be accepted in medicine. The 21(S) prolongation of coagulation time of whole blood (CT) is twice as long as 21 (R) 's, prolongation of recalcif ication time (RT) is three times of 21 (R) 's, extending prothrombin time (PT) is twice as 21 (R) 's, prolongation of thrombin time (TT) is little stronger than 21 (R) and prolongation of kaolin partial thromboplastin time (APTT) is twice as 21(R). Anticoagulation action of 21(S) Argatroban is 2-3 times of 21(R). Therefore, the 21 (S) isomer of Argatroban can be used as a new generation of direct thrombin inhibitor.</p> |
