专利号:US-6413785-B1 优先权日:1998-02-20 标题:Solid phase synthesis of 1-aminohydantoins 发明人:WILSON LAWRENCE JOSEPH; PORTLOCK DAVID EDWARD; LI MIN 权利人:PROCTER & GAMBLE 摘要:The subject invention involves processes for making 1-aminohydantoin compounds using a solid support resin, comprising the following steps; (a) preparing a resin-bound protected α-hydrazinyl ester; (1) by reacting the resin with an α-bromo carboxylic acid, then with a protected hydrazine; or (2) by reacting the resin with a protected α-hydrazinyl carboxylic acid; (b) preparing a resin-bound imine by removing the blocking group from the hydrazinyl moiety, then reacting the unprotected hydrazinyl moiety with an aldehyde or ketone; (c) preparing a resin-bound secondary urea: (1) by reacting the imine with p-nitrophenylchloroformate or trisphosgene, then with a primary amine; or (2) by reacting the imine with an isocyanate, and (d) preparing the 1-aminohydantoin compound by removing the secondary urea from the resin and cyclizing it.
专利号:AU-2181199-A 优先权日:1998-02-20 标 题 :Solid phase synthesis of 1-aminohydantoins
专利号:WO-2013023155-A1 优先权日:2011-08-11 标 题:Anhydrous and hemihydrate crystalline forms of an (r)-baclofen prodrug, methods of synthesis and methods of use
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合成参考文献
参考文献:10.1080/14756366.2022.2070909 摘要:Kaur S, Nieto NS, McDonald P, Beck JR, Honzatko RB, Roy A, Nelson SW. Discovery of small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase. Journal of Enzyme Inhibition and Medicinal Chemistry. 2022 May 05;37(1):1320–6. doi: 10.1080/14756366.2022.2070909.