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-5436368-A 优先权日:1990-10-31 标题:Intermediates in the preparation of 4,5-difluoroanthranillic acid 发明人:BRAISH TAMIM F 权利人:PFIZER 摘要:Compounds of the formula ##STR1## which are intermediates in the preparation of 4,5-difluoroanthranilic acid, an intermediate itself in the synthesis of quinolone antibacterials, and methods of preparing these intermediates.
专利号:EP-0332033-A2 优先权日:1988-03-11 标 题:N-cyclopropyl anilines and their use in processes for the synthesis of 1-cyclopropyl-quinolone-carboxylic acids and their derivatives 发明人:SCHRIEWER MICHAEL DR; PETERSEN UWE DR; GROHE KLAUS DR; KREBS ANDREAS DR 权利人:BAYER AG 摘要:N-Cyclopropylanilines of the formula (IV) in which R<1>, X<1>, X<2>, X<3>, A, Z and R<2> have the meaning given in the description, which are suitable for the preparation of 4-quinolone- 3-carboxylic acids, and processes for the preparation of quinolone- carboxylic acid derivatives using N-cyclopropylanilines.
专利号:US-6849650-B2 优先权日:1998-02-27 标 题:Heterocyclic compounds, pharmaceutical compositions comprising same, and methods for inhibiting β-amyloid peptide release and/or its synthesis by use of such compounds 发明人:THORSETT EUGENE D; PORTER WARREN J; NISSEN JEFFREY S; LATIMER LEE H; AUDIA JAMES E; DROSTE JAMES 权利人:ATHENA NEUROSCIENCES INC; LILLY CO ELI 摘要:Disclosed are compounds which inhibit β-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits β-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.
专利号:US-6399628-B1 优先权日:1996-11-22 标 题 :N-(aryl/heteroaryl) amino acid esters, pharmaceutical compositions comprising same, and methods for inhibiting alpha- amyloid peptide release and/or its synthesis by use of such compounds 发明人:AUDIA JAMES E; FOLMER BEVERLY K; JOHN VARGHESE; LATIMER LEE H; NISSEN JEFFREY S; REEL JON K; THORSETT EUGENE D; WHITESITT CELIA A 权利人:ATHENA NEUROSCIENCES INC; LILLY CO ELI 摘要:Disclosed are compounds which inhibit β-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits β-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.
专利号:EP-0951466-B1 优先权日:1996-12-23 标题:Cycloalkyl, lactam, lactone and related compounds, pharmaceutical compositions comprising same, and methods for inhibiting beta-amyloid peptide release and/or its synthesis by use of such compounds 发明人:WU JING; TUNG JAY S; THORSETT EUGENE D; PLEISS MICHAEL A; NISSEN JEFFREY S; NEITZ JEFFREY; LATIMER LEE H; JOHN VARGHESE; FREEDMAN STEPHEN; BRITTON THOMAS C; AUDIA JAMES E; REEL JON K; MABRY THOMAS E; DRESSMAN BRUCE A; CWI CYNTHIA L; DROSTE JAMES J; HENRY STEVEN S; MCDANIEL STACEY L; SCOTT WILLIAM L; STUCKY RUSSELL D 权利人:ELAN PHARM INC; LILLY CO ELI 摘要:Disclosed are compounds for Formula (I) wherein the substituents are as defined in the claims which inhibit β-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits β-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.
摘要:Silva, V. L. M.; Pinto, D. C. G. A.; Santos, C. M. M.; Rocha, D. H. A., Science of Synthesis Knowledge Updates, (2022) 3, 262. 摘要:Sharma, U.; Kumar, R.; Gupta, S. S.; Chandra, D., Science of Synthesis Knowledge Updates, (2022) 2, 247. 摘要:Sharma, U.; Kumar, R.; Gupta, S. S.; Chandra, D., Science of Synthesis Knowledge Updates, (2022) 2, 248. 参考文献:10.1016/j.ijantimicag.2007.12.007 摘要:Murugesan D, Palaniappan S, Perumal Y, Arnab C, Valakunja N, Sriram D. Antimycobacterial and phototoxic evaluation of novel 6-fluoro/nitro-4-oxo-7-(sub)-4H-[1,3]thiazeto[3,2-a]quinoline-3-carboxylic acid. International Journal of Antimicrobial Agents. 2008 Apr;31(4):337–44. doi: 10.1016/j.ijantimicag.2007.12.007. 参考文献:10.1107/s1600536810024189 摘要:Fu XS, Yu XP, Wang WM, Lin F. N-(3,4-Difluoro-phen-yl)phthalimide. Acta Crystallogr Sect E Struct Rep Online. 2010 Jun 26;66(Pt 7):o1809.