4 results about "Argatroban" patented technology

The application discloses an anticoagulant biomaterial for blood purification and a preparation method and application thereof, and comprises the following steps: providing an amphiphilic copolymer P(AA-MMA); blending polyethersulfone, P(AA-MMA) and a solvent, stirring at a set temperature to obtain a casting solution, and preparing a blending membrane from the casting solution; soaking the blending membrane in a 2-morpholine-4-yl ethanesulfonic acid buffer solution containing argatroban, 1-ethyl-(3-dimethylaminopropyl) carbonyl diimide and hydroxy succinimide, and reacting at room temperature to obtain an argatroban grafted blending membrane, namely the anticoagulant biomaterial. The method improves the hydrophilicity of the membrane, reduces the albumin adsorption of the membrane, reduces the adhesion of platelets on the membrane, prolongs the coagulation time APTT, PT and TT of the membrane, and is better in biocompatibility and enhanced in anticoagulation performance.

The application belongs to the technical field of medicine synthesis, and particularly relates to a preparation method of an intermediate 4-methyl-2-piperidinecarboxylic acid ethyl ester of argatroban. The application takes SM-1 as a starting material, realizes single bromination of an alpha position of a carbonyl group of the SM-1, and prepares a target compound through a rearrangement reaction. Compared with the prior art, the application can effectively avoid the use of a toxic cyanide in the prior art, can avoid a catalytic hydrogenation reaction, is safe in operation, can effectively reduce production cost, and is suitable for industrialized scale production.

This invention relates to the field of biomedical polymer materials technology, specifically to a polyethersulfone-based material with blood purification and anticoagulation functions, its preparation method, and its applications. The polyethersulfone-based material uses polyethersulfone as the main component, and a stable multi-coordination network structure is constructed by introducing terpyridine ligands and multivalent metal ions at the molecular level. Furthermore, the anticoagulant active molecules argatroban or heparin are immobilized on its surface, achieving selective adsorption of blood toxins and synergistic regulation of the anticoagulation reaction. The material is prepared using a process combining phase inversion membrane formation technology and surface coordination modification, resulting in a composite interface on the membrane surface rich in hydrophilic groups and a stable anticoagulant layer, significantly improving blood compatibility and membrane flux stability. This composite membrane can simultaneously perform purification and anticoagulation functions in hemodialysis, hemofiltration, and extracorporeal circulation systems, exhibiting good mechanical strength, chemical stability, and biosafety. The preparation route of this invention is simple, the parameters are controllable, and it is suitable for large-scale production.

The invention discloses a preparation method of an argatroban intermediate, and relates to the field of medicine synthesis. According to the method, N-Boc-N '-nitro-L-arginine and ethyl (2R, 4R)-4-methyl-2-piperidinecarboxylate are used as raw materials, 2-chloro-4, 6-dimethoxy-1, 3, 5-triazine is used as a condensing agent, in the presence of organic alkali N-methylmorpholine, a reaction is performed in a solvent, and the compound is obtained. According to the present invention, the argatroban intermediate (R)-4-methyl-1-(N8-nitro-N2-Boc-L-arginyl)-2-ethyl piperidinecarboxylate is obtained, the condensing agent and the introduced impurities adopted by the preparation method are easy to remove, the post-treatment operation is simple, the product yield is high, the purity is high, the residual condensing agent and the residual by-product in the product are easy to detect and control, and the argatroban intermediate (R)-4-methyl-1-(N8-nitro-N2-Boc-L-arginyl)-2-ethyl piperidinecarboxylate is suitable for commercial production.