专利号:US-6423877-B1 优先权日:1999-11-15 标题:Synthesis of pseudopterosin compounds 发明人:COREY ELIAS J 权利人:HARVARD COLLEGE 摘要:The present invention is directed to a new synthetic route to pseudopterosin aglycone (3): n a key intermediate for the synthesis of a group of antiinflammatory natural products including pseudopterosin A (1) and E (2). The pathway of synthesis starts with the abundant and inexpensive (S)-(−)-limonene and its long-known cyclic hydroboration product (4) and leads to the chiral hydroxy ketone (6). Conversion of (6) to (10) followed by a novel aromatic annulation produced (15) which underwent highly diastereoselective cyclization to afford the protected pseudopterosin aglycone (16). The naturally occurring pseudopterosins such as (1) and (2) are readily available from this key intermediate.
专利号:US-8106031-B2 优先权日:2006-05-02 标题:Hydrolytically-resistant boron-containing therapeutics and methods of use 发明人:LEE VING; PLATTNER JACOB J; BENKOVIC STEPHEN J; BAKER STEPHEN J; MAPLES KIRK R; BELLINGER-KAWAHARA CAROLYN; AKAMA TSUTOMU; ZHANG YONG-KANG; SINGH RAJESHWAR; SAURO VITTORIO A 权利人:LEE VING; PLATTNER JACOB J; BENKOVIC STEPHEN J; BAKER STEPHEN J; MAPLES KIRK R; BELLINGER-KAWAHARA CAROLYN; AKAMA TSUTOMU; ZHANG YONG-KANG; SINGH RAJESHWAR; SAURO VITTORIO A; ANACOR PHARMACEUTICALS INC 摘要:Compositions and methods of use of boron derivatives, including benzoxaboroles, benzazaboroles and benzthiaboroles, as therapeutic agents for treatment of diseases caused by fungi, yeast, bacteria or viruses are disclosed, as well as methods for synthesis of said agents and compositions thereof.
专利号:US-10287225-B2 优先权日:2015-05-13 标 题:Chain multiyne compound, preparation method and application thereof 发明人:XIA HAIPING; ZHUO QINGDE; LIN JIANFENG; ZHOU XIAOXI; CHEN ZHIXIN; SHAO YIFAN; ZHANG HONG; HE XUMIN 权利人:UNIV XIAMEN 摘要:The present invention relates to fields of organic chemistry and organometallic chemistry. The present invention discloses a chain multiyne compound, a preparation method thereof and an application in synthesizing a fused-ring metallacyclic compound. A structure of the chain multiyne compound in the present invention is shown as Formula I below. The present invention also provides a preparation method of the chain multiyne compound and an application thereof in a synthesis of a fused-ring metallacyclic compound. The chain multiyne compound disclosed in the present invention has multiple functional groups and the structure of the chain multiyne compound is adjustable. The chain multiyne compound can also be used to synthesize the fused-ring metallacyclic compound efficiently. The preparation method of the chain multiyne compound disclosed in the present invention is simple, which can be used to prepare the chain multiyne compound rapidly and efficiently.
专利号:US-9707301-B2 优先权日:2011-10-14 标题 :Pyrrolobenzodiazepines and targeted conjugates 发明人:JEFFREY SCOTT; BURKE PATRICK; HOWARD PHILIP WILSON 权利人:SEATTLE GENETICS INC; MEDIMMUNE LTD 摘要:This invention relates to pyrrolobenzodiazepines (PBDs), in particular pyrrolobenzodiazepine dimers having a C2-C3 double bond and an aryl group at the C2 position in each monomer unit, and their inclusion in targeted conjugates. The differing substituent groups may offer advantages in the preparation and use of the compounds, particularly in their biological properties and the synthesis of conjugates, and the biological properties of these conjugates.
专利号:GB-2080335-A 优先权日:1980-07-15 标题 :Electrochemical synthesis of organic compounds
专利号:EP-2558445-B1 优先权日:2010-04-15 标 题 :Intermediates useful for the synthesis of pyrrolobenzodiazepines
1: Kano K, Kitae T, Shimofuri Y, Tanaka N, Mineta Y. Complexation of polyvalent cyclodextrin ions with oppositely charged guests: entropically favorable complexation due to dehydration. Chemistry. 2000 Aug 4;6(15):2705-13. R., McKeon, J. E., & Ream, B. C. (1968). Palladium-catalyzed synthesis of benzyl esters from methyl-benzenes. The Journal of Organic Chemistry, 33(11), 4123-4127. 3: Field, F. H. (1969). Chemical ionization mass spectrometry. X. Temperature studies with substituted benzyl acetates. Journal of the American Chemical Society, 91(23), 6334-6341. 4: Okada, T., & Kamiya, Y. (1981). The liquid-phase oxidation of methylbenzenes by the cobalt-copper-bromide system. Bulletin of the Chemical Society of Japan, 54(9), 2724-2727.
合成参考文献
摘要:Gosmini, C.; Corpet, M., Science of Synthesis: Cross Coupling and Heck-Type Reactions, (2012) 1, 690. 参考文献:10.1038/nchem.1506 摘要:Over B, Wetzel S, Grütter C, Nakai Y, Renner S, Rauh D, Waldmann H. Natural-product-derived fragments for fragment-based ligand discovery. Nat Chem. 2013 Jan;5(1):21–8. doi: 10.1038/nchem.1506.