专利号:US-6720439-B1 优先权日:2001-09-28 标题:Synthesis of ruthenium-hydride complexes and preparation procedures of chiral alcohols and ketones 发明人:OHKUMA TAKESHI; KOIZUMI MASATOSHI; MUNIZ KILIAN; NOYORI RYOJI 权利人:INST NAGOYA IND SCIENCE RES 摘要:trans-RuH(eta<1>-BH4)[(S)-xylbinap][(S,S)-dpen] (0.00125 mmol), acetophenone (5.0 mmol), and 2-propanol (2.5 mL) were placed in an autoclave, and the resulting solution was repeatedly subject 5 times to a procedure of performing pressure reduction and argon introduction while stirring the solution for deaeration. A hydrogen tank was then connected to the autoclave, and after replacing the air inside an introduction tube with hydrogen, the pressure inside the autoclave was adjusted to 5 atmospheres and then hydrogen was released until the pressure dropped to 1 atmosphere. After repeating this procedure 10 times, the hydrogen pressure was adjusted to 8 atmospheres and stirring at 25° C. was performed for 12 hours. By concentrating the solution obtained by depressurization and subjecting the crude product to simple distillation, (R)-1-phenylethanol (yield: 95%) in the form of a colorless oily substance was obtained at an ee of 99%.
专利号:US-6005103-A 优先权日:1993-11-19 标题 :Pyrone derivatives as protease inhibitors and antiviral agents 发明人:DOMAGALA JOHN MICHAEL; LUNNEY ELIZABETH; PARA KIMBERLY SUZANNE; PRASAD JOSYULA VENKATA NAGENDR; TAIT BRADLEY DEAN 权利人:WARNER LAMBERT CO 摘要:The present invention relates to novel tri- and tetrasubstituted pyrones and related structures which potently inhibit the HIV aspartyl protease blocking HIV infectivity. The pyrone derivatives are useful in the development of therapies for the treatment of bacterial and viral infections and diseases, including AIDS. The present invention is also directed to methods of synthesis of multifunctionalized pyrones and of related structures.
专利号:EP-0729465-B1 优先权日:1993-11-19 标 题:Pyrone derivatives as protease inhibitors and antiviral agents 发明人:DOMAGALA JOHN MICHAEL; LUNNEY ELIZABETH; PARA KIMBERLY SUZANNE; PRASAD JOSYULA VENKATA NAGENDR; TAIT BRADLEY DEAN 权利人:PARKE DAVIS & CO 摘要:The present invention relates to novel tri- and tetrasubstituted pyrones and related structures which potently inhibit the HIV aspartyl protease blocking HIV infectivity. The pyrone derivatives are useful in the development of therapies for the treatment of bacterial and viral infections and diseases, including AIDS. The present invention is also directed to methods of synthesis of multifunctionalized pyrones and of related structures.
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