专利号:US-5861532-A 优先权日:1997-03-04 标 题:Solid-phase synthesis of N-alkyl amides 发明人:BROWN EDWARD G; NUSS JOHN M 权利人:CHIRON CORP 摘要:Methods for solid phase synthesis of N-alkyl amides comprise reductive amination of carbonyl compounds using a reducing agent and an amine-containing linker bound to a solid support. The methods afford high yields of linker-bound, monoalkylated amines, and subsequent coupling with acid derivatives provide derivatized N-substituted amides in excellent yields after cleavage from the solid-phase. Compositions useful in solid phase synthesis are also described.
专利号:US-2005130221-A1 优先权日:2001-02-01 标 题:Synthesis for the preparation of compounds for screening as potential tubulin binding agents 发明人:FLYNN BERNARD L; HAMEL ERNEST 权利人:US GOV HEALTH & HUMAN SERV 摘要:The present invention relates to methods for the synthesis of chemical compounds for screening as potential tubulin polymerization inhibitors. The invention also provides chemical compounds with tubulin polymerization inhibitor activity.
专利号:US-7468438-B2 优先权日:2004-03-25 标题:Process for the semisynthesis of deserpidine 发明人:FONTANA GABRIELE; BOMBARDELLI EZIO; SAMORI CRISTIAN; BALDELLI ELEONORA; GUERRINI ANDREA; BATTAGLIA ARTURO; DANIELI BRUNO 权利人:INDENA SPA 摘要:The present invention relates to an efficient procedure for the synthesis of deserpidine (Ia), starting from reserpic acid lactone (II) via the intermediate 11-O-demethyl reserpic acid lactone (III).
专利号:US-2016194279-A1 优先权日:2012-12-09 标 题 :One pot process for the conversion of aroyl chlorides to acyl thioureas 发明人:CHEPURI VENKATA RAMANA; BEERAN SENTHILKUMAR 权利人:COUNCIL SCIENT IND RES 摘要:The present invention disclose an improved one pot process for synthesis of acyl thioureas of formula (I), with yield greater than 80%, from aroyl chlorides of formula (I) wherein, R′ is an aryl or a heteroarylene group substituted with one or more groups selected from hydrogen, alkyl, alkylene, alkynyl, alkoxy, alkenyloxy, halo, hydroxyl, nitro, amino, carboxyl, ester, halogenated hydrocarbon or an aryl or heteroaryl; R″ and R′″ are selected independently from hydrogen, alkyl, alkylene, alkynyl, alkoxy, alkenyloxy, halo, hydroxyl, nitro, amino or halogenated hydrocarbon.
专利号:US-2022402908-A1 优先权日:2019-07-08 标题 :Cxcr6 inhibitors and methods of use 发明人:PEDDIBHOTLA SATYAMAHESHWAR; HERSHBERGER PAUL M; KIRBY RICHARD JASON; MALANY SIOBHAN; SMITH LAYTON H; MALONEY PATRICK R; SESSIONS HAMPTON; DIVLIANSKA DANIELA; PINKERTON ANTHONY B 权利人:SANFORD BURNHAM PREBYS MEDICAL DISCOVERY INST 摘要:Provided herein are small molecule inhibitors of CXCR6 receptor, compositions comprising the compounds, and methods of using the compounds and compositions. The compounds are 9-azbicyclo[3.3.1]nonane or 9-diazbicyclo[3.3.1]nonane derivatives, whose synthesis is also described. Also provided are method of treating a disease or condition (such as, cancer) mediated by CXCR6/CXCL16 signaling pathway in a mammal.
专利号:US-8536205-B2 优先权日:2005-05-25 标 题 :Photochromic and electrochromic compounds and synthesis and use thereof 发明人:BRANDA NEIL R; WUESTENBERG BETTINA; LEMIEUX VINCENT; ADAMS MICHAEL; GAUTHIER SIMON 权利人:BRANDA NEIL R; WUESTENBERG BETTINA; LEMIEUX VINCENT; ADAMS MICHAEL; GAUTHIER SIMON; SWITCH MATERIALS INC 摘要:Photochromic and electrochromic hexadiene compounds that are reversibly convertible between ring-open and ring-closed isomeric forms. The conversion between the different isomeric forms may be induced by light or electricity. The compounds may include a charge transfer moiety including electron donor and acceptor groups. The electron donor and acceptor are linearly conjugated in the ring-open form to enable electron transfer but are electrically insulated in the ring-closed form. Photoresponsive compounds may be synthesized by any of several methods disclosed, e.g., by reacting diene precursors with dienophiles in a condensation reaction. The compounds may be utilized in reactivity-gated photochromic or electrochromic applications. Compounds may be used in a method to selectively release a releasable agent, such as a small molecule.
参考标题:Microwave-Assisted Efficient Synthesis Of Polymethoxyacetophenones And Natural Polymethoxyflavones, And Their Inhibitory Effects On Melanogenesis 作者:Masao Tsukayama,Eiji Kusunoki,Mohammad M. Hossain,Yasuhiko Kawamura,Shinji Hayashi 摘要:Microwave-Assisted Friedel-Crafts Acetylation Of Polymethoxybenzenes With Acetic Anhydride In The Presence Of In(Cf 3 So 3 ) 3 Under Solvent-Free Conditions Was Achieved Rapidly To Give Polymethoxyacetophenones In High Yields. Microwave-Assisted Benzoylation Of 2'-Hydroxypolymethoxyacetophenones With Polymethoxybenzoyl Chlorides, Followed By The Rearrangement Of The Resulting Benzoates And The Final
合成参考文献
摘要:Mérour, J.-Y.; Joseph, B., Science of Synthesis Knowledge Updates, (2016) 3, 362. 摘要:Mérour, J.-Y.; Joseph, B., Science of Synthesis Knowledge Updates, (2016) 3, 316. 摘要:Waldvogel, S. R., Science of Synthesis Knowledge Updates, (2010) 1, 491. 摘要:Pitaval, A.; Echavarren, A. M., Science of Synthesis: Cross Coupling and Heck-Type Reactions, (2012) 1, 611. 摘要:Liu, S.; Xiao, J., Science of Synthesis: Cross Coupling and Heck-Type Reactions, (2012) 3, 255.