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伏立诺他的合成方法研究

study on synthetic method of Vorinostat
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摘要 伏立诺他(vorinostat),化学名为N、羟基、N'、苯基辛二酰胺,首个组蛋白脱乙酰酶抑制剂类抗肿瘤药。本文以辛二酸为初始原料,与乙酸酐脱水得辛二酸酐,再经酰胺化,酯化,羟胺化一共四步反应得到目标化合物——伏立诺他,总收率达到71.5%。 Vorinostat,the chemical name for it is N-hydroxy-N'-phenyl suberic acid,is the first antineoplastic drug of histone deacetylase inhibitor.Suberic acid was selected as the start material,suberic acid anhydride was prepared with acetic anhydride by the dehydration reaction.Then,the vorinostat was obtained through amidation,estertfication and hydroxylamine process.The total yield is 71.5%.
出处 《化工中间体》 2014年第9期38-41,共4页
关键词 伏立诺他 组蛋白脱乙酰酶抑制剂 T淋巴细胞瘤 合成 vorinostat histone deacetylase inhibitor T lymphocyte tumor synthetic
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参考文献9

  • 1焦杰,徐文方.抗肿瘤药Vorinostat的合成[J].中国医药工业杂志,2009,40(2):86-87. 被引量:7
  • 2张兴锴,孙铁民.治疗皮肤癌新药vorinostat[J].中国药物化学杂志,2007,17(4):268-268. 被引量:10
  • 3Sakura Sakajiri,Takashi Kumagai,Norihiko Kawamata,Takayuki Saitoh,Jonathan W. Said,H. Phillip Koeffler.Histone deacetylase inhibitors profoundly decrease proliferation of human lymphoid cancer cell lines[J]. Experimental Hematology . 2005 (1)
  • 4Antonello Mai,Monica Esposito,Gianluca Sbardella,Silvio Massa.A NEW FACILE AND EXPEDITIOUS SYNTHESIS OF N-HYDROXY-N’-PHENYLOCTANEDIAMJDE, A POTENT INDUCER OF TERMINAL CYTODIFFERECNTIATION[J]. Organic Preparations and Procedures International . 2001 (4)
  • 5Cohen Leonard A,Marks Paul A,Rifkind Richard A,Amin Shantu,Desai Dhimant,Pittman Brian,Richon Victoria M.Suberoylanilide hydroxamic acid (SAHA), a histone deacetylase inhibitor, suppresses the growth of carcinogen-induced mammary tumors. Anticancer Research . 2002
  • 6Chanaz Salmi-Smail,Aure?lie Fabre,Franck Dequiedt,Audrey Restouin,Re?my Castellano,Slaveia Garbit,Philippe Roche,Xavier Morelli,Jean Michel Brunel,Yves Collette.Modified Cap Group Suberoylanilide Hydroxamic Acid Histone Deacetylase Inhibitor Derivatives Reveal Improved Selective Antileukemic Activity. Journal of Medicinal Chemistry . 2010
  • 7John C. Stowell,Rachel I. Huot,Lainie Van Voast.The Synthesis of N-Hydroxy-N’-phenyloctanediamide and Its Inhibitory Effect on Proliferation of AXC Rat Prostate Cancer Cells. Journal of Medicinal Chemistry . 1995
  • 8Gediya Lalji K,Chopra Pankaj,Purushottamachar Puranik,Maheshwari Neha,Njar Vincent C O.A new simple and high-yield synthesis of suberoylanilide hydroxamic acid and its inhibitory effect alone or in combination with retinoids on proliferation of human prostate cancer cells. Journal of Medicinal Chemistry . 2005
  • 9Breslow R,M arks PA,Rifkind BA,et al.Novel potent inducers ofterminal differentiation and methods of use thereof (P). WO:9307148 . 1993

二级参考文献15

  • 1Richon VM, Emiliani S, Verdin E, et al. A class of hybridpolar inducers of transformed cell differentiation inhibits histone deacetylases [J]. Proc Natl Acad Sci USA, 1998, 95 (6) : 3003-3007.
  • 2Mark PA. Discovery and development of SAHA as an anticancer agent [J]. Oncogene, 2007, 26 (9) : 1351-1356.
  • 3FDA Approves New Drug for Skin Cancer, Zolinza [EB/OL]. [2006-10-06]. http://www.fda.gov/bbs/topics/ news/2006/new01484.html.
  • 4Breslow R, Marks PA, Rifkind BA, et al. Novel potent inducers of terminal differentiation and methods of use thereof: WO, 9307148 [P]. 1993-04-15.
  • 5Stowell JC, Huot RI, van Voast L, et al. The synthesis of N-hydroxy-N'-phenyloctanediamide and its inhibitory effect on proliferation of AXC rat prostate cancer cells [J]. J Med Chem, 1995, 38(9): 1411-1413.
  • 6Sbardella EG, Massa S. A new facile and expeditious synthesis of N-hydroxy-N'-phenyloctanediamide, a potent inducer of terminal cytodifferentiation [J]. OrgPrep Proced lnt, 2001, 33 (4) : 391-394.
  • 7Gediya LK, Chopra P, Purushottamachar P, et al. A new simple and high-yield synthesis of suberoylanilide hydroxamic acid and its inhibitory effect alone or in combination with retinoids on proliferation of human prostate cancer cells [J]. J Med Chem, 2005, 48(15): 5047-5051.
  • 8U.S.FDA.FDA approves vorinostat (Zolinza) for the treatment of cutaneous manifestations of cutaneous T-cell lymphoma(CTCL)[EB/OL].[2006-10-06].http://www.fda.gov/bbs/topics/NEWS/2006/NEW01484.html.
  • 9Merck & Co Inc.Preparation of tetrahydronaphthalene hydroxamates and benzamides as histone deacetylase(HDAC) inhibitors,EP:1541549[P].2005-06-15.
  • 10GEDIYA L K,et al.A new simple and high-yield synthesis of suberoylanilide hydroxamic acid and its inhibitory effect alone or in combination with retinoids on proliferation of human prostate cancer cells[J].J Med Chem,2005,48 (15):5047 -5051.

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