专利号:US-6632942-B2 优先权日:2000-05-04 标题:Asymmetric synthesis of piperazic acid and derivatives thereof 发明人:ROBIDOUX ANDREA L C; SERAFINI SIRO; DIETERICH PETRA; LEONARDI STEFANIA; STIBBARD JOHN 权利人:VERTEX PHARMA 摘要:This invention provides a concise, asymmetric synthesis of piperazic acid and derivatives thereof, whereby either the (3S)- or (3R)-enantiomeric form may be obtained with high optical purity. (3S)-piperazic acid is derived from D-glutamic acid through an (R)-2,5-dihydroxyvalerate ester intermediate. After the hydroxy groups are converted to suitable leaving groups, such as mesylates, the ester is treated with a bis-protected hydrazine to provide the desired (3S)-piperazic acid derivative. The (3R) enantiomer of piperazic acid may be similarly obtained starting with L-glutamic acid. The method may also be used to obtain piperazic acid derivatives that have moderate optical purity or are racemic. By this method, piperazic acid derivatives may be obtained that are useful as intermediates for pharmacologically active compounds. For example, certain intermediates of this invention are useful for preparing caspase inhibitors, particularly inhibitors of ICE, through additional steps known in the art.
专利号:US-7495100-B2 优先权日:2004-05-07 标题 :Synthesis of indenoisoquinolines 发明人:CUSHMAN MARK S; MORRELL ANDREW E; POMMIER YVES G 权利人:PURDUE RESEARCH FOUNDATION; US HEALTH 摘要:Indenoisoquinolines and dihydroindenoisoquinolines are described. In particular, such compounds possessing one or more electron withdrawing substituents are described. The in vitro anticancer activities of these molecules tested in the National Cancer Institute's screen of 55 cell lines is described. The compounds tested for topoisomerase I (top1) inhibition is described.
专利号:US-7741489-B2 优先权日:2007-03-30 标题:Process for the synthesis of solifenacin 发明人:PUIG SERRANO JORDI; CAMPS PELAYO 权利人:MEDICHEM SA 摘要:The present invention provides an improved synthetic strategy for the preparation of solifenacin and pharmaceutically acceptable salts thereof.
专利号:US-8378099-B2 优先权日:1994-10-28 标 题:Boronic ester and acid compounds, synthesis and uses 发明人:ADAMS JULIAN; MA YU-TING; STEIN ROSS L; BAEVSKY MATTHEW; GRENIER LOUIS; PLAMONDON LOUIS 权利人:MILLENNIUM PHARMACUETICALS INC; ADAMS JULIAN; STEIN ROSS L; BAEVSKY MATTHEW; GRENIER LOUIS; PLAMONDON LOUIS 摘要:Disclosed herein is a method for reducing the rate of degradation of proteins in an animal, comprising contacting cells of the animal with certain boronic ester and acid compounds. Also disclosed herein are novel boronic ester and acid compounds, their synthesis and uses.
专利号:US-2003176691-A1 优先权日:2000-05-04 标 题:Asymmetric synthesis of piperazic acid and derivatives thereof
专利号:US-2006025595-A1 优先权日:2004-05-07 标 题 :Synthesis of indenoisoquinolines
摘要:F. Holmes and W. R. C. Crimmin, J. Chem. Soc. 1955, 1175. 摘要:Li, Y.; Fang, X.; Wang, Y., Science of Synthesis: DNA-Encoded Libraries, (2024) nan, 17.