1-[3-(乙酰基氧基)-1-氮杂啶]乙酮置于盐酸体系中,用 水 用作溶剂,化学反应 4.0H,以100%的收率获得3-羟基氮杂环丁烷盐酸盐 参考文献:Acylative Dealkylation Of N-Tert-Butyl-3-Substituted Azetidines: Facile Access To [1.1.0]Azabicyclobutane,3-Hydroxyazetidinium Hydrochloride,And 3-Azetidinones 标题:Acylative Dealkylation Of N-Tert-Butyl-3-Substituted Azetidines: Facile Access To [1.1.0]Azabicyclobutane,3-Hydroxyazetidinium Hydrochloride,And 3-Azetidinones 摘要:A Novel Acylative Dealkylation Of N-Tert-Butylazetidines And Its Application To The Facile High-Yield Syntheses Of [1.1.0]Azabicyclobutane,3-Hydroxyazetidinium Hydrochloride,And 3-Azetidinones Is Described. Doi:10.1021/jo9602579
专利号:US-7825244-B2 优先权日:2005-06-10 标题:Intermediates useful in the synthesis of alkylquinoline and alkylquinazoline kinase modulators, and related methods of synthesis 发明人:BAINDUR NAND; GAUL MICHAEL DAVID; KREUTTER KEVIN DOUGLAS; XU GUOZHANG 权利人:JANSSEN PHARMACEUTICA NV 摘要:The invention is directed to alkylquinoline and alkylquinazoline compounds of Formula C: n nwherein R 1 , R 2 , R 99 , and X are as defined herein, the use of such compounds in the synthesis of protein tyrosine kinase inhibitors, particularly inhibitors of FLT3 and/or c-kit and/or TrkB.
专利号:US-9388147-B2 优先权日:2009-11-13 标题 :Selective sphingosine 1 phosphate receptor modulators and methods of chiral synthesis 发明人:MARTINBOROUGH ESTHER; BOEHM MARCUS F; YEAGER ADAM RICHARD; TAMIYA JUNKO; HUANG LIMING; BRAHMACHARY ENUGURTHI; MOORJANI MANISHA; TIMONY GREGG ALAN; BROOKS JENNIFER L; PEACH ROBERT; SCOTT FIONA LORRAINE; HANSON MICHAEL ALLEN 权利人:RECEPTOS INC; CELGENE INTERNAT II SÃ?RL 摘要:Compounds that selectively modulate the sphingosine 1 phosphate receptor are provided including compounds which modulate subtype 1 of the S1P receptor. Methods of chiral synthesis of such compounds are provided. Uses, methods of treatment or prevention and methods of preparing inventive compositions including inventive compounds are provided in connection with the treatment or prevention of diseases, malconditions, and disorders for which modulation of the sphingosine 1 phosphate receptor is medically indicated.
专利号:US-2014371464-A1 优先权日:2012-02-03 标 题:Process for the preparation of chiral isoxazoline azetidine derivatives as antiparasitic agents 发明人:BILLEN DENIS; GREENWOOD SEAN DAVID WILLIAM; STUK TIMOTHY LEE 权利人:ZOETIS LLC 摘要:The invention recites a chiral process for the synthesis of isoxazoline azetidine phenyl substituted derivatives of Formula (1) stereoisomers thereof, veterinarily acceptable salts thereof, processes for making, and their use as a parasiticide in an animal. The variables *, R 1a , R 1b , R 1c , R 2 , and R 3 are as described herein
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-9676783-B2 优先权日:2008-10-22 标 题:Method of treatment using substituted pyrazolo[1,5-A] pyrimidine compounds 发明人:HAAS JULIA; ANDREWS STEVEN W; JIANG YUTONG; ZHANG GAN 权利人:ARRAY BIOPHARMA INC 摘要:Compounds useful in the synthesis of compounds for treating pain, cancer, inflammation, neurodegenerative disease or Typanosoma cruzi infection in a mammal.
专利号:US-2007021436-A1 优先权日:2005-06-10 标 题 :Intermediates useful in the synthesis of alkylquinoline and alkylquinazoline kinase modulators, and related methods of synthesis
[参考文献]: Beck A, Et Al. Strategies And Challenges For The Next Generation Of Antibody-Drug Conjugates. Nat Rev Drug Discov. 2017;16(5):315-337. [参考文献]: Nalawansha Da, Et Al. Protacs: An Emerging Therapeutic Modality In Precision Medicine. Cell Chem Biol. 2020;27(8):998-985.
合成参考文献
摘要:Kleemann A., Kutscher B., Reichert D., Bossart M., Pharmaceutical Substances, Thieme [Online], Stuttgart, (2025).