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MGCD0103的合成 被引量：3

Synthesis of MGCD0103
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摘要 3-乙酰基吡啶经缩合、环合、氯代及胺化制得4-[[4-(3-吡啶基)嘧啶-2-氨基]甲基]苯甲酸甲酯,再经水解和缩合制得组蛋白去乙酰化酶抑制剂MGCD0103,总收率约26%(以3-乙酰基吡啶计),纯度99.4%。 The histone deacetylase inhibitor MGCD0103 was synthesized from 3-acetylpyridine by condensation, cyclization, chlorination and amination to give methyl 4- [[4- （3-pyridinyl） pyrimidin-2-ylamino] methyl] benzoate, which was subjected to hydrolysis and condensation with an overall yield of about 26% （based on 3-acetylpyridine） and purity of 99.4%.
作者 黄道伟 马志龙 张庆伟 张越 李建其
机构地区 中国医药工业研究总院上海医药工业研究院化学制药新技术中心 河北科技大学化学与制药工程学院
出处 《中国医药工业杂志》 CAS CSCD 北大核心 2012年第12期968-970,共3页 Chinese Journal of Pharmaceuticals
关键词 抗肿瘤药 组蛋白去乙酰化酶抑制剂 MGCD0103 合成 antitumor agent histone deacetylase inhibitor MGCD0103 synthesis
分类号 R979.19 [医药卫生—药品]
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参考文献8

  • 1谢华峰,陆涛.抗肿瘤药物组蛋白去乙酰化酶抑制剂的研究进展(上)[J].中国药师,2010,13(6):805-807. 被引量：5
  • 2白慧颖,胡森,冀文茹.组蛋白去乙酰化酶抑制剂的研究进展[J].感染．炎症．修复,2009,10(3):187-189. 被引量：3
  • 3Sung V, Richard N, Brady H, et al. Histone deacetylase inhibitor MGCD0103 synergizes with gemcitabine in human pancreatic cells [J]. Cancer Sci, 2011, 102 (6) : 1201-1207.
  • 4Zhou N, Moradei O, Raeppel S, et al. DiScovery of N- (2-aminophenyl) -4- E (4-pyridin-3-ylpyrimidin-2- ylamino) methyl:benzamide (MGCD0103), an orally active histone deacetylase inhibitor [J]. JMed Chem, 2008, 51 (14) : 4072-4075.
  • 5Liu YF, Wang CL, Bai Y J, et al. A facile total synthesis of imatinib base and its analogues [J]. Org Process Res Dev, 2008, 12 (3) : 490-495.
  • 6Huang A, Liu X, Lior Z. Novel process for preparing imatinib: US, 2006149061 [P]. 2006-07-06. (CA2006, 145: 124614).
  • 7Liu Z J, Vors JP, Gesing ERF, et al. Ligand-free copper- catalyzed amination of heteroaryl halides with alkyl and arylamines [J]. Adv Synth Catal, 2010, 352 (18) : 3158-3162.
  • 8Danel D, Zhou Z. Inhibitors of histone deacetylase: US, 2004142953 [P]. 2004-07-22. (CA 2004, 141: 140470).

二级参考文献31

  • 1周鹏,徐运.神经退行性疾病中的乙酰化内稳态[J].生命的化学,2006,26(6):541-543. 被引量：2
  • 2Mahlknecht U, Hoelzer D. Histone aeetylation modifiers in the pathogensis of malignant disease. Mol Med,2000, 6(8):623-644.
  • 3Kramer OH, Gottlicher M, Heinzel T. Histone deacetylase as a therapeutic target. Trends Endocrinol Metab,2001, 12(7) 1294-300.
  • 4Xu WS, Parmigiani RB, Marks PA. Histone deacetylase inhibitors: molecular mechanisms of action. Oncogene, 2007, 26(37) : 5541-5552.
  • 5Budillion A, Bruzzese F, Di Gennaro, et al. Multiple-target drugs: inhibitors of heat shock protein 90 and histone deacetylase. Curr Drug Targets,2005, 6(3):337-351.
  • 6Leng Y, Chuang DM. Endogenous alpha-synuclein is induced by valproic acid through histone deacetylase inhibition and participates in neuroprotection against glutamate induced excitotoxicity. J Neurosci,2006, 26(28) :7502-7512.
  • 7Ren M, Leng Y, Jeong M, et al. Valproic acid reduces brain damage induced by transient focal cerebral ischemia in rats: potential roles of histone deacetylase inhibition and heat shock protein induction. J Neurochem, 2004, 89(6):1358-1367.
  • 8Li Y, Yuan Z, Liu B, et al. Prevention of hypoxia-induced neuronal apoptosis through histone deacetylase inhibition. J Trauma, 2008, 65(4):863-870.
  • 9Sinn DI, Kim SJ, Chu K,et al. Valproie acid-mediated neuroprotection in intracerebral hemorrhage via histone deacetylase inhibition and transcriptional activation. Neurobiol Dis, 2007, 26 (2) : 464-472.
  • 10Kim HJ, Rowe M, Ren M, etal. Histone deacetylase inhibitors exhibit anti-inflammatory and neuroprotective effects in a rat permanent ischemic model of stroke: multiple mechanisms of action. J Pharmacol Exp Ther, 2007, 321(3) :892-901.

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中国医药工业杂志
2012年 第12期

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