CAS: 125533-88-2; Mofarotene

该化合物是合成的视质素,一种与维生素A有关的化合物,以其调节细胞生长和差异的能力而闻名,具有各种皮肤病症和某些类型癌症治疗的兴趣,其功能主要是通过激活对硫酸受体(RARs)来发挥的,影响基因表达和细胞过程,其化学结构包括一系列交融的双联结,有助于其生物活动和稳定性. 摩拉多丁通常在主题上或系统上管理,视所治疗的条件而定. 该化合物在治疗的皮肤病症(如皮丝病)及其抗发炎效应方面的潜力已经进行了研究. 但是,与其他对类素一样,该化合物可能具有副作用,包括皮肤刺激和致畸性,因此有必要仔细考虑其使用,特别是在孕妇身上.

结构式图片

MSDS等安全信息

    合成工艺路线路线简述

      📜6-溴-1,1,4,4-四甲基-1,2,3,4-四氢化萘,乙烯基硼酸频哪醇酯,4-(2-(4-(Chloromethyl)Phenoxy)Ethyl)Morpholine置于[ni(μ-Cl)(Ipr)]2,三氟甲磺酸三甲基硅酯,四丁基溴化铵,三乙胺,Potassium Phosphate,Tris-(Dibenzylideneacetone)Dipalladium(0),三苯基膦体系中,用 甲苯,N,N-二甲基甲酰胺 用作溶剂,化学反应 24.0H,以32%的收率获得莫法罗汀
      参考文献:镍催化苄基化和烯烃异构化立体选择性合成三取代烯烃
      标题:镍催化苄基化和烯烃异构化立体选择性合成三取代烯烃
      摘要:Nhc-Ni I催化剂促进极化末端烯烃与氯化苄的区域选择性和立体选择性偶联,得到三取代的硼烯和苯乙烯.该反应通过支链选择性 Heck 型苄基化,然后是反式选择性烯丙基异构化.
      Doi:10.1002/anie.202202674

      海关参考信息

      专利信息


      专利号:US-8734846-B2
      优先权日:2008-06-16
      标 题 :Methods for the preparation of targeting agent functionalized diblock copolymers for use in fabrication of therapeutic targeted nanoparticles
      发明人:ALI MIR M; HRKACH JEFF; ZALE STEPHEN E; ALVAREZ DE CIENFUEGOS LUIS
      权利人:BIND BIOSCIENCES INC
      摘要:This application provides nanoparticles and methods of making nanoparticles using pre-functionalized poly(ethylene glycol)(also referred to as PEG) as a macroinitiator for the synthesis of diblock copolymers. Ring opening polymerization yields the desired poly(ester)-poly (ethylene glycol)-targeting agent polymer that is used to impart targeting capability to therapeutic nanoparticles. This “polymerization fromâ€? approach typically employs precursors of the targeting agent wherein the reactivity of functional groups of the targeting agent is masked using protecting groups. Also described is a “coupling toâ€? that utilized the poly(ethylene glycol)-targeting agent conjugate where the targeting agent remains in its native un-protected form. This method uses “orthogonalâ€? chemistry that exhibit no cross reactivity towards functional groups typically found within targeting agents of interest.

      专利号:US-2013035307-A1
      优先权日:2010-01-26
      标 题:Methods for treating or preventing the spread of cancer using semi-synthetic glycosaminoglycosan ethers
      发明人:PRESTWICH GLENN D; KENNEDY THOMAS P
      权利人:UNIV UTAH RES FOUND; PRESTWICH GLENN D; KENNEDY THOMAS P
      摘要:Described herein are methods for the treatment and prevention of tumor metastasis using alkylated and fluoroalkylated semi-synthetic glycosaminoglycan ethers (“SAGEsâ€?). The synthesis of sulfated alkylated and fluoroalkylated SAGEs is also described.

      专利号:US-2008214827-A1
      优先权日:2004-02-03
      标 题:Synthesis of Cyanoimino-Benzoimidazoles
      发明人:GOEHRING R RICHARD; WHITEHEAD JOHN; SHAO BIN
      权利人:EURO CELTIQUE SA
      摘要:Disclosed in certain embodiments is a process for synthesizing a compound of formula (V) and salts thereof.

      专利号:US-9220714-B2
      优先权日:2006-03-16
      标 题 :Nitrofuran compounds for the treatment of cancer and angiogenesis
      发明人:SAULNIER SHOLLER GISELLE L; SWAMY NARASIMHA; KALKUNTE STAYAN; SINGH RAKESH K; BRARD LAURENT; KIM KYU KWANG
      权利人:WOMEN AND INFANTS HOSPITAL OF RHODE ISLAND; UNIV BROWN; WOMEN AND INFANTS HOSPITAL RHODE ISLAND
      摘要:The invention is directed to the synthesis and use of nitrofuran compounds, especially Nifurtimox, as medicaments to treat cancer, especially neuroblastoma, and to inhibit angiogenesis. The invention also provides compositions, unit dosage forms, and kits comprising the compounds.

      专利号:US-2024382626-A1
      优先权日:2023-05-16
      标题 :Irradiation amenable liposomal dye aggregates and methods of synthesis and use thereof
      发明人:PORTER TYRONE; STERN NOAH; TUNNELL JAMES; SHRESTHA BINITA
      权利人:UNIV TEXAS
      摘要:The present invention provides lipid nanoparticles that are amenable to an irradiation at a wavelength at or above 850 nm, have an absorption peak from about 850 to 1100 nm wavelength, and comprise a high transition temperature lipid and a dye (e.g., a J-aggregate of a dye). In some embodiments, the dye (e.g., J-aggregate of the dye) is encapsulated in the lipid nanoparticle. In various embodiments, the present invention also relates to compositions comprising said lipid nanoparticles and methods of generating said lipid nanoparticles and compositions thereof. The present invention further relates to methods relating to the said lipid nanoparticles for imaging, detection, and treatment of diseases or disorders (e.g., phototherapy) in a subject.

      专利号:US-2008281105-A1
      优先权日:2005-01-18
      标题:Novel Quinolinium Salts and Derivatives
      发明人:MACDONALD JAMES E; HYSELL MICHELLE K; YU DEHUA; LI HENRY; WONG-STAAL FLOSSIE
      权利人:IMMUSOL INC
      摘要:The present invention relates generally to the synthesis of novel quinolinium salts and derivative compounds. Such salts and compounds are useful for inhibiting the growth of cancer cells.

      供应商参考报价(招募中)

      品牌试剂参考报价(招募中)

      📌 第三方产品分析报告

      ✅ COA系统入驻 | 共享模式

      主要参考文献


      1: Lave T, Schmitt-Hoffmann AH, Coassolo P, Valles B, Ubeaud G, Ba B, Brandt R, Chou RC. A new extrapolation method from animals to man: application to a metabolized compound, mofarotene. Life Sci. 1995;56(26):PL473-8.
      15: López-Boado YS, Klaus M, Dawson MI, López-Otín C. Retinoic acid-induced expression of apolipoprotein D and concomitant growth arrest in human breast cancer cells are mediated through a retinoic acid receptor RARalpha-dependent signaling pathway. J Biol Chem. 1996 Dec 13;271(50):32105-11. Review.
      20: Rao GN, Ney E, Herbert RA. Effect of retinoid analogues on mammary cancer in transgenic mice with c-neu breast cancer oncogene. Breast Cancer Res Treat. 1998 Apr;48(3):265-71.

      合成参考文献


      参考文献:10.1182/blood.v88.8.3147.bloodjournal8883147
      摘要:Pomponi F, Cariati R, Zancai P, De Paoli P, Rizzo S, Tedeschi R, Pivetta B, De Vita S, Boiocchi M, Dolcetti R. Retinoids irreversibly inhibit in vitro growth of Epstein-Barr virus- immortalized B lymphocytes. 1996 Oct 15;88(8):3147–59. doi: 10.1182/blood.v88.8.3147.bloodjournal8883147.
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