CAS: 471905-41-6; 3-(Cis-4-((4-Chlorophenyl)Sulfonyl)-4-(2,5-Difluorophenyl)Cyclohexyl)Propanoic Acid

该化合物是一种合成有机化合物,其特点是复杂的分子结构,包括环形环和各种功能组;存在一个磺酰集团和多种氟原子,有助于其独特的化学特性,如脂质增加和潜在的生物活动;由于"精密"的配置,该化合物有可能表现出特定的立体化学特性,影响其与生物目标的相互作用;可能对其在制药中的潜在应用进行研究,特别是在开发防炎剂或止炎剂方面.氯联苯和二氟苯替代成分可能增强它与某些受体或酶的结合性.与含有卤素和磺基化合物的许多化合物一样,有必要考虑其稳定性,溶性以及在不同条件下的再活性.由于某些成分具有潜在的毒性,安全和处理防范措施是必要的.

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CAS号656810-86-5 cis-1-[4-[(4-ch... | CAS号7758-19-2 亚氯酸钠 | CAS号5329-14-6 氨基磺酸 | CAS号106-54-7 4-氯苯硫酚 | CAS号470716-52-0 2-[[(4-氯苯基)硫代]甲... | CAS号470716-51-9 2-((4-氯苯基磺酰基)甲基... | CAS号85117-99-3 2,5-二氟溴苄 | CAS号471903-20-5 4-[(4-氯苯基)磺酰基]-... | CAS号471905-61-0 2-{1-[(4-Chloro...

合成工艺路线路线简述

  • 合成目标产物 Cis-4-[(4-Chlorophenyl)Sulfonyl]-4-(2,5-Difluorophenyl)Cyclohexanepropanoic Acid 主要起始原料 3-((1S,4R)-4-(4-Chlorophenylsulfonyl)-4-(2,5-Difluorophenyl)Cyclohexyl)Propanal And Sodium Chlorite And Sulfamic Acid
  • (文献来源)合成步骤主要原料 3-((1S,4R)-4-(4-Chlorophenylsulfonyl)-4-(2,5-Difluorophenyl)Cyclohexyl)Propanal 和 Sodium Chlorite 和 Sulfamic Acid
📜Cis-4-[(4-Chlorophenyl)Sulfonyl]-4-(2,5-Difluorophenyl)Cyclohexanepropanal置于sodium Chlorite,氨基磺酸体系中,用 二氯甲烷,水 作为反应溶剂,化学反应 0.5H,以74%的收率获得产物顺式-4-[(4-氯苯基)磺酰基]-4-(2,5-二氟苯基)环己烷丙酸
参考文献: Synthesis Of Cyclohexanone Derivatives[fr] Synthese De Derives De Cyclohexanone
标题: Synthesis Of Cyclohexanone Derivatives[fr] Synthese De Derives De Cyclohexanone
摘要:本文介绍了一种制备环己酮(1)的新工艺.所得产品可用作γ-分泌酶抑制剂,或作为合成其他γ-分泌酶抑制剂的中间体.

海关参考信息

专利信息


专利号:US-7276637-B2
优先权日:2002-08-02
标题:Synthesis of cyclohexanone derivatives
发明人：BRANDS KAREL MARIE JOSEPH; DAVIES ANTONY JOHN; OAKLEY PAUL JOSEPH; SCOTT JEREMY PETER; SHAW DUNCAN EDWARD; TEALL MARTIN RICHARD
权利人:MERCK & CO INC
摘要:A novel process for preparing cyclohexanone derivatives of formula (I) n nis described. The products are useful as gamma secretase inhibitors, or as intermediates in the synthesis of other gamma secretase inhibitors.

专利号:US-7411088-B2
优先权日:2004-02-20
标 题:Stereoselective synthesis of a 4,4-disubstituted cyclohexanepropanoic acid
发明人：BRANDS KAREL MARIE JOSEPH; BREWER SARAH ELIZABETH; DAVIES ANTONY JOHN; DOLLING ULF H; HAMMOND DEBORAH CAMILLE; LIEBERMAN DAVID ROSS; SCOTT JEREMY PETER
权利人:MERCK & CO INC; MERCK SHARP & DOHME
摘要:There is provided stereoselective route to a compound of formula I: n nwherein R represents H or an alkali metal, Ar 1 represents 4-chlorophenyl and Ar 2 represents 2,5-difluorophenyl.

专利号:US-2007225520-A1
优先权日:2004-02-20
标题 :Stereoselective Synthesis of a 4,4-Disubstituted Cyclohexanepropanoic Acid

专利号:US-2005222456-A1
优先权日:2002-08-02
标 题:Synthesis of cyclohexanone derivatives

专利号:WO-2004013090-A1
优先权日:2002-08-02
标题 :Synthesis of cyclohexanone derivatives

专利号:EP-1718593-B1
优先权日:2004-02-20
标题:Stereoselective synthesis of a 4,4-disubstituted cyclohexanepropanoic acid

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主要参考文献


1: Bai F, Tagen M, Colotta C, Miller L, Fouladi M, Stewart CF. Determination of the gamma-secretase inhibitor MK-0752 in human plasma by online extraction and electrospray tandem mass spectrometry (HTLC-ESI-MS/MS). J Chromatogr B Analyt Technol Biomed Life Sci. 2010 Sep 1;878(25):2348-52. Epub 2010 Jul 30.
2: Cook JJ, Wildsmith KR, Gilberto DB, Holahan MA, Kinney GG, Mathers PD, Michener MS, Price EA, Shearman MS, Simon AJ, Wang JX, Wu G, Yarasheski KE, Bateman RJ. Acute gamma-secretase inhibition of nonhuman primate CNS shifts amyloid precursor protein (APP) metabolism from amyloid-beta production to alternative APP fragments without amyloid-beta rebound. J Neurosci. 2010 May 12;30(19):6743-50.
3: Matthews CZ, Woolf EJ. Determination of a novel gamma-secretase inhibitor in human plasma and cerebrospinal fluid using automated 96 well solid phase extraction and liquid chromatography/tandem mass spectrometry. J Chromatogr B Analyt Technol Biomed Life Sci. 2008 Feb 15;863(1):36-45. Epub 2008 Jan 6. Review.

合成参考文献


摘要:S55 | ZINC15PHARMA | Pharmaceuticals from ZINC15 | DOI:10.5281/zenodo.3247749
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