CAS: 5373-42-2; Thalicarpine

该化合物是来自Thalitrum植物的碱性物质,以其在Thalitrum 种中的存在而著称,其特点是复杂的双环结构,其中包括一个结合的等离子线框架.该化合物展示了一系列生物活动,包括潜在的止痛和抗炎特性,使其对药理研究感兴趣. (+)-Thallicarpine通常被发现为白色到白色以外的晶体状固体,其溶液因溶剂而异,其溶液往往比水中有机溶剂更溶.该化合物的立体化学特性很重要,因为(+)名称表明其特定的光学活动,可以影响其生物相互作用.此外,(+)-Thaliccarpine已经研究过它对各种生物系统的影响,包括其在调制...

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      专利号:US-3875167-A
      优先权日:1972-05-26
      标 题 :Synthesis of thalicarpine
      发明人:KUPCHAN S MORRIS; LIEPA ANDRIS J
      权利人:RESEARCH CORP
      摘要:There is disclosed a novel total synthesis of thalicarpine which includes inter alia a total synthesis of hernandaline. The novel process is characterised in utilizing simple and readily available starting materials to form a diaryl ether system which is then condensed with a 3,4-dihydroisoquinolinium salt which is then converted to hernandaline. Hernandaline is reacted with a bicyclic Reissert compound to yield a compound having the thalicarpine skeleton, nascent hydrogen reduction yields Nmonodesmethyl thalicarpine which is methylated.

      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-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.

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      主要参考文献


      1: Wu WN, McKown LA. The in vitro metabolism of thalicarpine, an aporphine-benzyltetrahydroisoquinoline alkaloid, in the rat. API-MS/MS identification of thalicarpine and metabolites. J Pharm Biomed Anal. 2002 Aug 22;30(1):141-50.

      合成参考文献


      摘要:National Cancer Institute Screening Program Data Summary, Developmental Therapeutics Program., JAN1986
      摘要:Progress Report Submitted to the National Cancer Institute by Arthur D. Little, Inc., -(60), 1969
      摘要:National Technical Information Service., PB82-166299
      摘要:Toxicology and Applied Pharmacology., 17(284), 1970
      参考文献:10.1248/yakushi1947.86.9_763
      摘要:Tomita M, Lu ST, Chen YY. [Alkaloids of Hernandia ovigera L]. Yakugaku Zasshi. 1966 Sep;86(9):763–6. doi: 10.1248/yakushi1947.86.9_763.
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