专利号:US-6252079-B1 优先权日:1993-06-30 标 题 :Intermediates in the synthesis of camptothecin and related compounds and synthesis thereof 发明人:CURRAN DENNIS P; BOM DAVID 权利人:UNIV PITTSBURGH 摘要:The present invention provides a short, convergent total synthesis of irinotecan and derivative compounds which comprises of a novel 4+1 radical annulation wherein the precursoris reacted with an aryl isonitrile having the formulawherein X is Br or I, and R4 is an alkyl group, an allyl group, a propargyl group or a benzyl group, and R16 is H, a C1-C6 alkoxy group, agroup wherein p is an integer between 4 and 12, or a C1-C12 acyclic dialkylamino group. The present invention also provides novel chemical intermediates for such 4+1 radical annulations.
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-5521310-A 优先权日:1992-10-07 标 题 :Process to obtain benzoxazines to be used for the synthesis of ofloxazine, levofloxazine and derivatives 发明人:CARRETERO GONZALVEZ JUAN-CARLO; VICIOSO SANCHEZ MERCEDES; GARCIA RUANO JOSE-LUIS 权利人:ETILO DERIVADOS 摘要:A process to obtain benzoxazines useful for the synthesis of Ofloxazine, Levofloxazine and derivatives. The benzoxacines (I) where Xb is an halogen and R 1 is H, alkyl or alkenyl of up to 6 atoms of C or aryl, can be obtained by means of cycling a compound of formula (II) through the reaction with triphenylphosphine and ethyl azodicarboxilate. The compounds of formula (II) can be obtained through the reaction of a compound (III) with an adequate epoxide. Through the use of the adequate chiral epoxide it is possible to obtain the enantiomerically desired intermediate and, therefore and selectively, it is possible to obtain the desired final product with the adequate enantiomeric form without the need to carry out a resolution stage. n The Compounds (I) are useful and key intermediates for the synthesis of the antimicrobials Oflixazine and Levofloxazine. ##STR1##
专利号:US-8877930-B2 优先权日:2009-11-04 标 题 :Continuous flow synthesis of amino alcohols using microreactors 发明人:BEDORE MATTHEW W; ZABORENKO NIKOLAY; JENSEN KLAVS F; JAMISON TIMOTHY F 权利人:BEDORE MATTHEW W; ZABORENKO NIKOLAY; JENSEN KLAVS F; JAMISON TIMOTHY F; MASSACHUSETTS INST TECHNOLOGY 摘要:The present invention provides various methods for the synthesis of chemical species in a microreactor environment. In some cases, reaction products of the present invention may be valuable as intermediates and/or products in pharmaceutical and polymer research. For example, the method may involve the synthesis of amino alcohols within a microchannel. Embodiment described herein may allow for reactions with significantly shorter reaction times and increased efficiency.
专利号:US-9688644-B2 优先权日:2009-04-30 标 题 :Synthesis of Tetracyclines and intermediates thereto 发明人:MYERS ANDREW G; KUMMER DAVID A; LI DERUN; HECKER EVAN; DION AMELIE; WRIGHT PETER M 权利人:HARVARD COLLEGE 摘要:The tetracycline class of antibiotics has played a major role in the treatment of infectious diseases for the past 50 years. However, the increased use of the tetracyclines in human and veterinary medicine has led to resistance among many organisms previously susceptible to tetracycline antibiotics. The recent development of a modular synthesis of tetracycline analogs through a chiral enone intermediate has allowed for the efficient synthesis of novel tetracycline analogs never prepared before. The present invention provides more efficient routes for preparing the enone intermediate and allows for substituents at positions 4a, 5, 5a, and 12a of the tetracycline ring system.
专利号:US-11059914-B2 优先权日:2016-12-21 标题:Method for the continuous synthesis of a diene elastomer with lithium amide initiator 发明人:DIRE CHARLOTTE; DESSENDIER MARIE-HÉLÈNE 权利人:MICHELIN & CIE 摘要:A process for the continuous synthesis of a diene elastomer is provided. The synthesis is conducted by means of n reactors r1 to rn, considered to be continuous stirred-tank reactors, which are equipped with an internal stirring system. The reactors are arranged in series, n varying from 2 to 15, preferably from 2 to 9. The reactor r1 is fed by an input solution comprising a solvent, one or more monomer(s), an anionic polymerization initiator chosen from lithium amides and a polar agent. The conversion by weight C1 in the first reactor is less than 70%, and the total conversion by weight Cn at the outlet of the reactor rn is greater than or equal to 70%.
[参考文献]: Alla V Lipeeva, Et Al. Synthesis Of 1H-1,2,3-Triazole Linked Aryl(Arylamidomethyl) - Dihydrofurocoumarin Hybrids And Analysis Of Their Cytotoxicity. Eur J Med Chem. 2015 Jul 15:100:119-28. [参考文献]: Almeqdad Y Habashneh, Et Al. Synthesis And Antitumor Activities Of Some New N1-(Flavon-6-Yl)Amidrazone Derivatives. Arch Pharm (Weinheim). 2014 Jun;347(6):415-22. [参考文献]: Amjad M Qandil, Et Al. The Hydrolysis Kinetics Of Monobasic And Dibasic Aminoalkyl Esters Of Ketorolac. Drug Dev Ind Pharm. 2013 Sep;39(9):1346-56. [参考文献]: H Welinder, Et Al. Ige Antibodies Against Piperazine And N-Methyl-Piperazine In Two Asthmatic Subjects. Int Arch Allergy Appl Immunol. 1986;79(3):259-62. [参考文献]: Jin-Ping Li, Et Al. The Pan-Inhibitor Of Aurora Kinases Danusertib Induces Apoptosis And Autophagy And Suppresses Epithelial-To-Mesenchymal Transition In Human Breast Cancer Cells. Drug Des Devel Ther. 2015 Feb 17:9:1027-62.
合成参考文献
参考文献:10.1007/s11010-011-0953-8 摘要:Makowska M, Łukowska-Chojnacka E, Wińska P, Kuś A, Bilińska-Chomik A, Bretner M. Design and synthesis of CK2 inhibitors. Molecular and Cellular Biochemistry. 2011 Jul 13;356(1-2):91. doi: 10.1007/s11010-011-0953-8.