1-甲基-3-(甲硫基)苯置于六甲基磷酰三胺,Sodium Hydride,二乙胺体系中,用 Xylene 用作溶剂,化学反应 6.0H,以92%的收率获得3-甲基苯硫酚 参考文献:Selective Dealkylation Of Alkyl Aryl Sulfides 标题:Selective Dealkylation Of Alkyl Aryl Sulfides 摘要: Doi:10.1055/s-1982-29868
专利信息
专利号:EP-1660469-B1 优先权日:2003-07-18 标题 :Process for the preparation of 11-(1-piperazinyl)dibenzo 'b, f! '1 ,4!-thiazepine, an intermediate in the synthesis of the antipsychotic drug quetiapine 发明人:KACZMAREK LUKASZ; BADOWSKA-ROSLONEK KATARZYNA; STOLARCZYK ELZBIETA; SZELEJEWSKI WIESLAW 权利人:HELM AG; INST FARMACEUTYCZNY 摘要:A process for the preparation of 11-(1-piperazinyl)dibenzo-[b, f ] [ 1, 4 ] thiazepine comprising reacting phenyl 2Â(phenylthio) phenylcarbamate with piperazine and cyclizing the obtained N-[ (2 -phenylthio) phenyl ] -1 -piperazinylcarboxamide in a presence of cyclizing agent. 11-(1-piperazinyl)-dibenzo [b, f] [1, 4]thiazepine is itself, an intermediate in the synthesis of antipsychotic drug Quetiapine.
专利号:US-5670465-A 优先权日:1993-01-08 标题 :Preparation of p-fuchsones and synthesis of p-dihydroxylated aromatic compounds therefrom 发明人:COSTANTINI MICHEL; MANAUT DANIEL; MICHELET DANIEL 权利人:RHONE POULENC CHIMIE 摘要:p-Dihydroxylated aromatic compounds are prepared via the oxidation of p-fuchsones, the latter advantageously being synthesized by reacting a phenolic compound having at least one hydrogen atom in the para-position to the hydroxyl function with a non-enolizable ketonic compound, in the presence of a catalytically effective amount of an acid catalyst and, optionally, a cocatalytically effective amount of an ionizable sulfur-containing compound.
专利号:US-6472531-B1 优先权日:1994-09-19 标题 :Synthesis of 3-[4-(2-aminoethoxy)-benzoyl]-2-aryl-6-hydroxybenzo[b]thiophenes 发明人:LABELL ELIZABETH SMITH; MCGILL JOHN MCNEILL; MILLER RANDAL SCOT 权利人:LILLY CO ELI 摘要:The present invention is directed to chemical processes for preparing 2-aryl-6-hydroxy-3-[4-(2-aminoethoxy)benzoyl]benzo[b]-thiophenes. The present invention is also directed to crystalline solvates and a non-solvated crystalline form of 6-hydroxy-2-(4-hydroxyphenyl)-3-[4-(2-piperidinoethoxy)benzoyl]-benzo[b]thiophene hydrochloride, as well as processes for their preparation.
专利号:US-2004053999-A1 优先权日:1997-09-17 标题 :Novel compounds and methods for synthesis and therapy 发明人:BISCHOFBERGER NORBERT W; DAHL TERRENCE C; HITCHCOCK MICHAEL J M; KIM CHOUNG U; LEW WILLARD; LIU HONGTAO; MILLS ROGER G; WILLIAMS MATTHEW A 摘要:Novel compounds are described. The compounds generally comprise an acidic group, a basic group, a substituted amino or N-acyl and a group having an optionally hydroxylated alkane moiety. Pharmaceutical compositions comprising the inhibitors of the invention are also described. Methods of inhibiting neuraminidase in samples suspected of containing neuraminidase are also described. Antigenic materials, polymers, antibodies, conjugates of the compounds of the invention with labels, and assay methods for detecting neuraminidase activity are also described.
专利号:US-6225341-B1 优先权日:1995-02-27 标 题:Compounds and methods for synthesis and therapy 发明人:BISCHOFBERGER NORBERT W; KIM CHOUNG U; LEW WILLARD; LIU HONGTAO; WILLIAMS MATTHEW A 权利人:GILEAD SCIENCES INC 摘要:Novel compounds are described. The compounds generally comprise an acidic group, a basic group, a substituted amino or N-acyl and a group having an optionally hydroxylated alkane moiety. Pharmaceutical compositions comprising the inhibitors of the invention are also described. Methods of inhibiting neuraminidase in samples suspected of containing neuraminidase are also described. Antigenic materials, polymers, antibodies, conjugates of the compounds of the invention with labels, and assay methods for detecting neuraminidase activity are also described.
专利号:US-5936128-A 优先权日:1993-11-19 标题:5,6-dihydropyrone derivatives as protease inhibitors and antiviral agents 发明人:ELLSWORTH EDMUND LEE; LUNNEY ELIZABETH; TAIT BRADLEY DEAN 权利人:WARNER LAMBERT CO 摘要:The present invention relates to novel 5,6-dihydropyrone derivatives and related structures which potently inhibit the HIV aspartyl protease blocking HIV infectivity. The 5,6-dihydropyrone derivatives are useful in the development of therapies for the treatment of bacterial and viral infections and diseases, including AIDS. The present invention is also directed to methods of synthesis of multifunctionalized 5,6-dihydropyrones and of related structures.
参考标题:Copper-Mediated Direct Sulfenylation Of 4-Hydroxyquinolinones And 4-Hydroxypyridones With Aryl Thiols Via A C−h Functionalization Process 作者:Tao Guo,Hongyan Wang |发布日期:2017.9 摘要:An Efficient Approach For The Direct Sulfanylation Of 4-Hydroxyquinolinones And 4-Hydroxypyridones With Aryl Thiols In The Presence Of Cui/dmso Has Been Developed. The Substrate Scope Is Broad, Allowing Facile Synthesis Of A Range Of Structurally Diverse 3-Sulfanyl-4-Hydroxyquinolinones And 3-Sulfanyl-4-Hydroxypyridones In Good Efficiency.
合成参考文献
摘要:Tsubouchi, A., Science of Synthesis Knowledge Updates, (2016) 2, 344. 摘要:Kashemirov, B. A.; Błażewska, K.; Justyna, K.; Lyu, J.; McKenna, C. E., Science of Synthesis Knowledge Updates, (2021) 1, 412. 摘要:Eichman, C. C.; Stambuli, J. P., Science of Synthesis: Cross Coupling and Heck-Type Reactions, (2012) 2, 383. 摘要:Sinha, A. K.; Singh, R., Science of Synthesis, (2021) , 519. 摘要:Sinha, A. K.; Singh, R., Science of Synthesis, (2021) , 497.