(2R,4R)-4-羟基哌啶-1,2-二羧酸1-叔丁酯2-甲酯 | 321744-25-6

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 中文名称: (2R,4R)-4-羟基哌啶-1,2-二羧酸1-叔丁酯2-甲酯
• 英文名称: (2R,4R)-methyl 1-(tert-butoxycarbonyl)-4-hydroxypiperidine-2-carboxylate
• 英文别名: 1-tert-butyl 2-methyl (2R,4R)-4-hydroxypiperidine-1,2-dicarboxylate；1-O-tert-butyl 2-O-methyl (2R,4R)-4-hydroxypiperidine-1,2-dicarboxylate
• CAS: 321744-25-6
• 化学式: C₁₂H₂₁NO₅
• 分子量: 259.302
• InChiKey: RNMVWSAJMIKMDY-RKDXNWHRSA-N

物化性质

• 密度：
  1.182

计算性质

• 辛醇/水分配系数(LogP)：
  0.9
• 重原子数：
  18
• 可旋转键数：
  4
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.83
• 拓扑面积：
  76.1
• 氢给体数：
  1
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  (2R,4R)-4-羟基哌啶-1,2-二羧酸1-叔丁酯2-甲酯 、 4-氯-7-甲氧基喹唑啉-6-醇 以to give 1-tert-butyl 2-methyl (2R,4S)-4-[(4-chloro-7-methoxyquinazolin-6-yl)oxy]piperidine-1,2-dicarboxylate (17)的产率得到1-tert-butyl 2-methyl (2R,4S)-4-[(4-chloro-7-methoxyquinazolin-6-yl)oxy]piperidine-1,2-dicarboxylate
  参考文献：
  名称：

  QUINAZOLINE DERIVATIVES AS TYROSINE KINASE INHIBITORS

  摘要：

  本发明涉及公式I的喹唑啉衍生物或其药学上可接受的盐：其中R1，R2，R3，R4和m的定义如描述中所定义；其制备方法；含有它们的制药组合物以及它们用于制造抗增殖效应药物的用途。公式I的喹唑啉衍生物预计可用于治疗某些由erbB受体酪氨酸激酶介导的癌症，例如EGFR酪氨酸激酶。

  公开号：

  US20110152297A1

文献信息

• QUINAZOLINE DERIVATIVES AS TYROSINE KINASE INHIBITORS
  申请人：Halsall Christopher Thomas

  公开号：US20110152297A1

  公开（公告）日：2011-06-23

  The invention concerns quinazoline derivatives of the Formula I, or pharmaceutically acceptable salts thereof: wherein each of R 1 , R 2 , R 3 , R 4 and m are as defined in the description; processes for their preparation; pharmaceutical compositions containing them and their use in the manufacture of a medicament for providing an anti-proliferative effect. The quinazoline derivatives of Formula I are expected to be useful in the treatment of diseases such as certain cancers mediated by erbB receptor tyrosine kinases, and, for example, EGFR tyrosine kinase.

  本发明涉及公式I的喹唑啉衍生物或其药学上可接受的盐：其中R1，R2，R3，R4和m的定义如描述中所定义；其制备方法；含有它们的制药组合物以及它们用于制造抗增殖效应药物的用途。公式I的喹唑啉衍生物预计可用于治疗某些由erbB受体酪氨酸激酶介导的癌症，例如EGFR酪氨酸激酶。
• DEUTERATED OMEGA DIPHENYLUREA RELATED COMPOUNDS AND INTERMEDIATES
  申请人：Suzhou Zelgen Biopharmaceutical Co., Ltd.

  公开号：US20140128612A1

  公开（公告）日：2014-05-08

  Methods and processes for preparation and production of deuterated ω-diphenylurea are disclosed. Especially, a kind of deuterated ω-diphenylurea compounds which can inhibit phosphokinase and the preparation method of N-(4-chloro-3-(trifluoromethyl)phenyl)-N′-(4-(2-(N-d3-methylcarbamoyl)-4-pridinyloxy)phenyl)urea are disclosed. The said deuterated diphenylurea compounds can be used for treating or preventing tumors and relative diseases.

  公开了制备和生产氘代ω-二苯基脲的方法和过程。特别是公开了一种可以抑制磷酸激酶的氘代ω-二苯基脲化合物以及N-(4-氯-3-(三氟甲基)苯基)-N′-(4-(2-(N-d3-甲基氨基)-4-吡啶氧基)苯基)脲的制备方法。所述氘代二苯基脲化合物可用于治疗或预防肿瘤及相关疾病。
• Constrained (l-)-S-adenosyl-l-homocysteine (SAH) analogues as DNA methyltransferase inhibitors
  作者：Ljubomir Isakovic、Oscar M. Saavedra、David B. Llewellyn、Stephen Claridge、Lijie Zhan、Naomy Bernstein、Arkadii Vaisburg、Nadine Elowe、Andrea J. Petschner、Jubrail Rahil、Norman Beaulieu、France Gauthier、A. Robert MacLeod、Daniel Delorme、Jeffrey M. Besterman、Amal Wahhab

  DOI：10.1016/j.bmcl.2009.03.132

  日期：2009.5

  Potent SAH analogues with constrained homocysteine units have been designed and synthesized as inhibitors of human DNMT enzymes. The five membered (2S,4S)-4-mercaptopyrrolidine-2-carboxylic acid, in 1a, was a good replacement for homocysteine, while the corresponding six-member counterpart was less active. Further optimization of 1a, changed the selectivity pro. le of these inhibitors. A Chloro substituent at the 2-position of 1a, compound 1d, retained potency against DNMT1, while N-6 alkylation, compound 7a, conserved DNMT3b2 activity. The concomitant substitutions of 1a at both 2- and N-6 positions reduced activity against both enzymes. (C) 2009 Elsevier Ltd. All rights reserved.
• US6399629B1
  申请人：——

  公开号：US6399629B1

  公开（公告）日：2002-06-04
• US8735410B2
  申请人：——

  公开号：US8735410B2

  公开（公告）日：2014-05-27