74863-82-4Relevant academic research and scientific papers
Preparation method of 3-methylquinoline-8-sulfonyl chloride
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Paragraph 0046-0049; 0058-0077, (2020/03/17)
The invention belongs to the field of fine chemical product production, and particularly relates to a preparation method of 3-methylquinoline-8-sulfonyl chloride, and the method comprises the following steps: (1) carrying out catalytic cyclization on 2-aminobenzene sulfonic acid serving as an initial raw material, propionaldehyde and paraformaldehyde in a deep eutectic solvent to obtain 3-methylquinoline-8-sulfonic acid; and (2) carrying out acylating chlorination on the generated 3-methylquinoline-8-sulfonic acid under the action of an organic alkali by using bis (trichloromethyl) carbonate as a chlorinating agent, thereby obtaining the 3-methylquinoline-8-sulfonyl chloride. The method has the advantages of simple operation process, easily available raw material, low cost, no generation of harmful gases in the whole process, meeting of safety and environmental protection requirements, and facilitation of large-scale production.
Aminoguanidines and alkoxyguanidines as protease inhibitors
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, (2008/06/13)
Aminoguanidine and alkoxyguanidine compounds, including compounds of the formula: wherein X is O or NR9and R114 R4, R6-R9, R11, R12, Ra, Rb, Rc, Y, Z, n and mare set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit proteolytic enzymes such as thrombin are described. Also described are methods for preparing the compounds of Formula I. The novel compounds of the present invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, thrombin, plasmin and factor Xa. Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of thrombin, or are intermediates useful for forming compounds having antithrombotic activity. The invention includes a composition for inhibiting loss of blood platelets, inhibiting formation of blood platelet aggregates, inhibiting formation of fibrin, inhibiting thrombus formation, and inhibiting embolus formation in a mammal, comprising a compound of the invention in a pharmaceutically acceptable carrier. Other uses of compounds of the invention are as anticoagulants either embedded in or physically linked to materials used in the manufacture of devices used in blood collection, blood circulation, and blood storage, such as catheters, blood dialysis machines, blood collection syringes and tubes, blood lines and stents.
HETEROAROMATIC AND THIOHETEROAROMATIC SUBSTITUTED SULFONAMIDE THROMBIN INHIBITORS
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, (2008/06/13)
Sulfonamide thrombin inhibitors are provided which have the structure STR1 including all stereoisomers thereof, wherein X is S or--CH 2--; m is 0, 1 or 2 when X is--S--or m is 0 when X is--CH. sub.2--; n is 1, 2 or 3; R 1 and R 2 are independently H, lower alkyl, cyclo-alkyl, aryl, heteroaryl or heteroarylalkyl, or R 1 and R 2 can be taken together with the N atom to which they are attached to form a 5-to 8-membered ring which may optionally contain an additional N, O or S atom in the ring; R. sup.3 is heteroaryl; and R 4 is alkyl, cycloalkyl, aryl, heteroaryl, quinolinyl or tetrahydroquinolinyl, and pharmaceutically acceptable salts thereof.
