📜1-苄基-3-(叔丁氧羰氨基)吡咯烷置于钯体系中,用 甲醇 作为反应溶剂,化学反应生成 3-(Boc-氨基)吡咯烷 参考文献:Process For The Synthesis Of 3-Chloro-2,4,5-Trifluorobenzoic Acid 标题:Process For The Synthesis Of 3-Chloro-2,4,5-Trifluorobenzoic Acid 摘要:描述了一种改进的制备3-氯-2,4,5-三氟苯甲酸的过程,涉及将3,4,5,6-四氟-1,2-苯二甲酸二酯与取代胺反应,得到3-氨基-2,4,5-三氟苯甲酸,随后将氨基中间体转化为3-氯-2,4,5-三氟苯甲酸.
专利号:US-6528517-B1 优先权日:1998-02-04 标题:Synthesis of quinobenzoxazine analogues with topoisomerase II and quadruplex interactions for use as antineoplastic agents 发明人:HURLEY LAURENCE H; ZENG QINGPING; KWOK YAN; GAM JONGSIK; KERWIN SEAN M 权利人:UNIV TEXAS 摘要:The present invention discloses a novel quinobenzoxazine self-assembly complex on DNA and on the topoisomerase II-DNA complex. The related model is used to design a new series of quinobenzoxazines, pyridobenzophenoxazines, pyrridonaphthophenoxazines, and other related compounds that may exhibit anticancer or antibiotic activity. The anticancer activity of these compounds is thought to operate via stabilization of the topoisomerase II-DNA complex and/or interaction with G-quadruplexes, while the antibiotic activity of these compounds derives from their ability to inhibit gyrase, the bacterial type II topoisomerase.
专利号:US-4885386-A 优先权日:1988-10-28 标题 :Process for the synthesis of 3-chloro-2,4,5-trifluorobenzoic acid 发明人:WEMPLE JAMES N; KARRICK GREGORY L; SPENCE FLOYD G 权利人:WARNER LAMBERT CO 摘要:An improved process for the preparation of 3-chloro-2,4,5-trifluorobenzoic acid is described which involves reaction of a diester of 3,4,5,6-tetrafluoro-1,2-benzenedicarboxylic acid with a substituted amine to afford 3-amino-2,4,5-trifluorobenzoic acid followed by subsequent conversion of the amio intermediate into 3-chloro-2,4,5-trifluorobenzoic acid.
专利号:US-8399502-B2 优先权日:2008-09-17 标 题 :Analogs of indole-3-carbinol and their use as agents against infection 发明人:JONG LING; JIANG FAMING; LI GAOQUAN; MORTELMANS KRISTIEN 权利人:JONG LING; JIANG FAMING; LI GAOQUAN; MORTELMANS KRISTIEN; STANFORD RES INST INT 摘要:Compounds useful as antibacterial agents are provided. The compounds are analogs of indole-3-carbinol and have a backbone selected from dihydroindolo[2,3-b]carbazole, 2,2′-diindolylmethane, 2′,3-diindolylmethane, and 3,3′-diindolylmethane. The compounds are useful therapeutic and prophylactic treatment of bacterial infections in mammals. Methods of synthesis of the compounds are provided, as are pharmaceutical compositions containing the compounds.
专利号:US-6797820-B2 优先权日:1999-12-17 标 题:Succinate compounds, compositions and methods of use and preparation 发明人:PATEL DINESH; JACOBS JEFFREY W; JAIN RAKESH; NI ZHI-JIE; YUAN ZHENGYU 权利人:VICURON PHARM INC 摘要:Novel hydroxamic acid compounds are disclosed. These hydroxamates inhibit peptidyl deformylase (PDF), an enzyme present in prokaryotes. The hydroxymates are useful as antimicrobials and antibiotics. The compounds of the invention display selective inhibition of peptidyl deformylase versus other metalloproteinases such as matrix metalloproteinases (MMPs). Methods of synthesis and of use of the compounds are also disclosed.
专利号:US-9868746-B2 优先权日:2012-02-23 标题:Substituted 5-aminothieno[2,3-C]pyridazine-6-carboxamide analogs as positive allosteric modulators of the muscarinic acetylcholine receptor M4 发明人:LINDSLEY CRAIG W; CONN P JEFFREY; WOOD MICHAEL R; MELANCON BRUCE J; TARR JAMES C; SALOVICH JAMES M; POSLUSNEY MICHAEL S 权利人:UNIV VANDERBILT 摘要:In one aspect, the invention relates to substituted 5-aminothieno[2,3-c]pyridazine-6-carboxamide analogs, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the muscarinic acetylcholine receptor M 4 (mAChR M 4 ); synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
专利号:WO-9940093-A2 优先权日:1998-02-04 标题 :Synthesis of quinobenzoxazine analogues with topoisomerase ii and quadruplex interactions for use as antineoplastic agents
[参考文献]: Takahiro Takayama, Et Al. A Novel Approach For Lc-Ms/ms-Based Chiral Metabolomics Fingerprinting And Chiral Metabolomics Extraction Using A Pair Of Enantiomers Of Chiral Derivatization Reagents. Anal Chim Acta. 2015 Oct 22:898:73-84.
合成参考文献
摘要:Spitzner, D., Science of Synthesis Knowledge Updates, (2016) 1, 79.