专利号:US-8101779-B2 优先权日:2008-10-06 标题 :Enantioselective synthesis of (+) and (–)-2-[1-(2,6-dichlorophenoxy)-ethyl]-1,3-diazacyclopent-2-ene 发明人:CROOKS PETER A; VARTAK ASHISH PRAMOD 权利人:CROOKS PETER A; VARTAK ASHISH PRAMOD; UNIV KENTUCKY RES FOUND 摘要:Methods for the enantioselective synthesis of (+) and (−) lofexidine or 2-[1-(2,6)-dichlorophenoxy)-ethyl]-1,3-diazacyclopent-2-ene involve converting (+) or (−) 1-methyl-1-[2,6-dichlorophenoxy]ethanamide to an (+) or (−) imino-ether intermediate by electrophilic attack of the amide oxygen by a trimethoxonium ion and, without isolation, converting the (+) or (−) imino-ether intermediate to (+) or (−) 2-[1-(2,6-dichlorophenoxy)-ethyl]1,3-diazacyclopent-2-ene by adding ethylene diamine; and optionally converting the (+) or (−) 2-[1-(2,6-dichlorophenoxy)-ethyl]1,3-diazacyclopent-2-ene into a pharmaceutically acceptable acid addition salt thereof.
专利号:US-4937367-A 优先权日:1987-07-15 标 题:Process for the preparation of intermediates for the synthesis of fosfomycin 发明人:CASTALDI GRAZIANO; GIORDANO CLAUDIO 权利人:ZAMBON SPA 摘要:A process is described for the preparation of intermediates useful in the synthesis of Fosfomycin. n More particularly, an enantioselective process is described for the preparation of derivatives of (1S,2S)-1,2-dihydroxypropyl-phosphonic acid of formula ##STR1## wherein R 2 and R 3 have the meanings reported in the specification.
专利号:US-4412958-A 优先权日:1981-10-16 标 题:Stereospecific synthesis of 5-phenyl-2S-pentanol 发明人:CUE JR BERKELEY W; MOORE BERNARD S 权利人:PFIZER 摘要:5-Phenyl-2S-pentanol is synthesized stereospecifically from S ethyl lactate. The method provides easily purified 5-phenyl-2S-pentanol useful in the synthesis of central nervous system active (CNS) agents such as levonantradol.
专利号:US-6384228-B2 优先权日:1998-05-26 标题 :Method for synthesis of halopyridyl-azacyclopentane derivative and intermediate thereof 发明人:NODE MANABU; NAKAMURA DAISAKU; FUJIWARA TOSHIO; ICHIHASHI SHOGO 权利人:NIHON MEDIPHYSICS CO LTD 摘要:The present invention relates to a method for synthesis of an optically active halopyridyl-azacyclo-pentane derivative and the intermediate thereof which comprises preparing an optically active allene-1,3-dicarboxylic acid ester derivative from an optically active acetonedicarboxylic acid ester derivative and then proceeding through a 7-azabicyclo[2.2.1]heptane derivative to obtain the objective product.
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-2018111938-A1 优先权日:2015-05-05 标 题:Synthesis of Intermediates Used in the Manufacture of Anti-HIV Agents 发明人:PRADHAN BRAJA SUNDAR; AMARNATH KOMMIREDDY; VEMPALA NARESH; RAHMAN MD ATAUR 权利人:CBZ INVEST LTD 摘要:The present invention relates to a process of preparing intermediates of Formula (I). The process comprises of reacting compound of Formula (III) with compound of Formula (V) in the presence of a solvent selected from an alcohol, ether or water to form compound of Formula (I) wherein, R 1 is selected from —NH 2 , Cl, Br, NHCOR″, wherein R″ is alkyl, aryl, Schiff's base of formula Nâ•?CHR′, wherein R′ is alkyl or aryl; R 2 is selected from H, alkyl; R 3 and R 4 , each independently is H; R 5 and R 6 , each independently is H, alkyl; R 7 is H, alkyl; and R 8 is H, alkyl.
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合成参考文献
摘要:Drabowicz, J.; Kiełbasiński, P.; Łyżwa, P.; Mikołajczyk, M.; Zając, A., Science of Synthesis, (2009) 42, 737. 摘要:Cunha, J. C.; Dedeiras, B.; Negrão, A. C. R.; Marques, M. M. B., Science of Synthesis: Hypervalent Halogens in Organic Synthesis, (2025) . 参考文献:10.1021/jo035435u 摘要:Kawaguchi T, Funamori N, Matsuya Y, Nemoto H. Total synthesis of macrosphelides A, B, and E: first application of ring-closing metathesis for macrosphelide synthesis. J Org Chem. 2004 Jan 23;69(2):505–9. doi: 10.1021/jo035435u.