CAS: 85754-59-2; Ambamustine

该化合物是一种合成烷基制剂,属于被称为氮芥子化合物类别,主要特征是能够与DNA形成共价联系,导致DNA复制和转录的交叉联系和随后抑制.这一机制使它成为潜在的乳胶化药剂,特别是治疗某些类型癌症.Ambamustaine展示了一种独特的结构,它结合了烷基剂和其他治疗方式的特征,这可能提高它的功效,减少与传统乳油类药物相比的副作用.其溶液性,稳定性和再活性受到其化学结构的影响,其中包括对其生物活动至关重要的氯乙基化合物.安巴穆斯丁的药用,毒性和治疗窗口正在研究,因为它有望改善癌症治疗结果.然而,与许多烷基剂一样,在临床应用中,必须认真考虑其潜在的副作用和抗药机制.

结构式图片

MSDS等安全信息

    合成工艺路线路线简述

      📜3-(P-Fluorophenyl)-N-Formyl-L-Alanyl-3--L-Alanyl-L-Methionine Ethyl Ester 反应生成 氨莫司汀
      参考文献:Debarbieri,A.;Bekesi,J. G.
      标题:Debarbieri,A.;Bekesi,J. G.

      海关参考信息

      专利信息


      专利号:US-12351573-B2
      优先权日:2019-05-09
      标 题:Compounds for use in synthesis of peptidomimetics
      发明人:AL-ABED YOUSEF; CHENG KAI FAN
      权利人:FEINSTEIN INSTITUTES FOR MEDICAL RESEARCH
      摘要:Synthesis of O-benzotriazole and O-imidazole synthons are described. Uses of synthons in synthesis of azapeptides and other peptidomimetics, azapeptides and other peptidomimetics synthesized from the synthons and uses of azapeptides and other peptidomimetics are also described.

      专利号:US-2023159450-A1
      优先权日:2020-05-08
      标 题 :Dimers for use in synthesis of peptidomimetics
      发明人:AL-ABED YOUSEF; ALTITI AHMAD
      权利人:FEINSTEIN INSTITUTES FOR MEDICAL RESEARCH
      摘要:Dimers for use in synthesis of peptidomimetics are described. Uses of dimers as synthons in synthesis of azapeptides and other peptidomimetics, azapeptides and other peptidomimetics synthesized from the dimers and uses of azapeptides and other peptidomimetics are also described.

      专利号:US-12391691-B2
      优先权日:2018-11-16
      标题:Synthesis of key intermediate of KRAS G12C inhibitor compound
      发明人:PARSONS ANDREW THOMAS; COCHRAN BRIAN MCNEIL; POWAZINIK IV WILLIAM; CAPORINI MARC ANTHONY
      权利人:AMGEN INC
      摘要:The present invention relates to an improved, efficient, scalable process to prepare intermediate compounds, such as compound 5M, having the structure n nuseful for the synthesis of compounds that target KRAS G12C mutations, such as

      专利号:US-2025206736-A1
      优先权日:2019-11-14
      标题 :Synthesis of kras g12c inhibitor compound
      发明人:CORBETT MICHAEL THOMAS; CAILLE SEBASTIEN
      权利人:AMGEN INC
      摘要:The present disclosure relates to an improved, efficient, scalable process to prepare intermediate compounds, such as 2-isopropyl-4-methylpyridin-3-amine, useful for the synthesis of compounds, such as Compound 9, for the treatment of KRAS G12C mutated cancers.

      专利号:US-2020354404-A1
      优先权日:2019-05-09
      标 题 :Peptidomimetic agents, synthesis and uses thereof
      发明人:AL-ABED YOUSEF
      权利人:FEINSTEIN INSTITUTES FOR MEDICAL RESEARCH
      摘要:Compounds for use in synthesis of peptidomimetic agents; synthesis of peptidomimetic agents; peptidomimetic diagnostic and therapeutic agents; and uses of the compounds and peptidomimetic agents in drug discovery, diagnosis, prevention and treatment of diseases are described.

      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.

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      📌 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: Ardizzoni A, Antonelli G, Ricci S, Frasci G, Rinaldi M, Boni L, Galletti P, Pennucci MC, Antonuzzo A, Gravina A, Galli L, Comella G, Conte PF, Salvati F, Rosso R. Ambamustine in the second-line treatment of patients with small-cell lung cancer: a phase II Fonicap study. Am J Clin Oncol. 2000 Feb;23(1):22-5. Italian. II. In vivo bioassay. Cancer Chemother Pharmacol. 1984;12(2):77-82.

      合成参考文献


      摘要:Yagi MJ, Maldarelli F, Chin SE, Holland JF, Bekesi JG. Interference of mouse mammary tumor virus replication by PTT.119 [p-fluoro-L-phe-m-bis-(2-chloroethyl)amino-L-phe-met ethoxy HCl]--an antitumor agent. J Natl Cancer Inst. 1986 Mar;76(3):493–501.
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