(+/-)-trans-3-(tert-butyl-dimethylsilanyloxy)-cyclopentylamine

• 分子结构分类: 有机化合物 - 有机金属化合物 - 有机类金属化合物
• 英文名称: (+/-)-trans-3-(tert-butyl-dimethylsilanyloxy)-cyclopentylamine
• 英文别名: (1R,3R)-3-[tert-butyl(dimethyl)silyl]oxycyclopentan-1-amine
• 化学式: C₁₁H₂₅NOSi
• 分子量: 215.411
• InChiKey: BFVALWDNFFRUCH-NXEZZACHSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.89
• 重原子数：
  14
• 可旋转键数：
  3
• 环数：
  1.0
• sp3杂化的碳原子比例：
  1.0
• 拓扑面积：
  35.2
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  (+/-)-trans-3-(tert-butyl-dimethylsilanyloxy)-cyclopentylamine 在 氢氟酸 、 N,N-二异丙基乙胺 作用下， 以 1,4-二氧六环 、 乙腈 为溶剂， 反应 5.0h， 生成 (Z)-4-(3-hydroxy-cyclopentylamino)-3-(3-methoxy-1H-pyrrol-2-ylmethylene)-5-nitro-2,3-dihydro-indol-2-one
  参考文献：
  名称：

  Synthesis of Potent Oxindole CDK2 Inhibitors

  摘要：

  A series of oxindole CDK2 inhibitors was synthesized. These novel analogues have a saturated monosubstituted cyclic moiety at their C-4 position that mimics the ribofuranoside of ATP. This substitution afforded agents with increased potency relative to the parent indolinone and nanomolar range IC50 against the CDK2 enzyme and two cancer cell lines. (C) 2003 Elsevier Science Ltd. All rights reserved.

  DOI：

  10.1016/s0968-0896(03)00036-1
• 作为产物：
  描述：

  syn-4-(tert-butyldimethylsilyloxy)cyclopentene oxide 在 platinum(IV) oxide 、 palladium on activated charcoal 二苯基膦叠氮化物 、 氢气 、 三苯基膦 、 偶氮二甲酸二乙酯 作用下， 以 四氢呋喃 、 乙醇 为溶剂， 20.0 ℃ 、101.33 kPa 条件下， 反应 74.0h， 生成 (+/-)-trans-3-(tert-butyl-dimethylsilanyloxy)-cyclopentylamine
  参考文献：
  名称：

  Synthesis of Potent Oxindole CDK2 Inhibitors

  摘要：

  A series of oxindole CDK2 inhibitors was synthesized. These novel analogues have a saturated monosubstituted cyclic moiety at their C-4 position that mimics the ribofuranoside of ATP. This substitution afforded agents with increased potency relative to the parent indolinone and nanomolar range IC50 against the CDK2 enzyme and two cancer cell lines. (C) 2003 Elsevier Science Ltd. All rights reserved.

  DOI：

  10.1016/s0968-0896(03)00036-1

文献信息

• RO4383596, an orally active KDR, FGFR, and PDGFR inhibitor: Synthesis and biological evaluation
  作者：Lee A. McDermott、Mary Simcox、Brian Higgins、Tom Nevins、Kenneth Kolinsky、Melissa Smith、Hong Yang、Jia K. Li、Yingsi Chen、June Ke、Navita Mallalieu、Tom Egan、Stan Kolis、Aruna Railkar、Louise Gerber、Kin-Chun Luk

  DOI：10.1016/j.bmc.2005.05.012

  日期：2005.8

  (+/-)-1-(anti-3-Hydroxy-cyclopentyl)-3-(4-methoxy-phenyl)-7-phenylamino-3,4-dihydro-1H-pyrimido[4,5-d]pyrimidin-2-one (RO4383596) is a potent and selective inhibitor of the pro-angiogenic receptor tyrosine kinases KDR, FGFR, and PDGFR. This agent has an excellent pharmacokinetic profile and is highly efficacious in rodent models of angiogenesis upon oral administration. (c) 2005 Elsevier Ltd. All rights reserved.

  (+/-)-1-(anti-3-羟基环戊基)-3-(4-甲氧基苯基)-7-苯基氨基-3,4-二氢-1H-吡咯并[4,5-d]嘧啶-2-酮（RO4383596）是一种高效且选择性作用于促血管生成的受体酪氨酸激酶KDR、FGFR和PDGFR的抑制剂。该药物具有优异的药代动力学特性，并且在啮齿类血管生成模型中表现出显著的疗效。© 2005 Elsevier Ltd. 保留所有权利。
• Pyrimido compounds having antiproliferative activity
  申请人：——

  公开号：US20040204427A1

  公开（公告）日：2004-10-14

  Disclosed are novel pyrimido compounds that are selective inhibitors of both KDR and FGFR kinases. These compounds and their pharmaceutically acceptable salts are anti-proliferative agents useful in the treatment or control of solid tumors, in particular breast, colon, lung and prostate tumors. Also disclosed are pharmaceutical compositions containing these compounds and methods of treating cancer.

  公开了新型的嘧啶化合物，它们是对KDR和FGFR激酶的选择性抑制剂。这些化合物及其药用可接受的盐类是抗增殖剂，在治疗或控制实体瘤，特别是乳腺癌、结肠癌、肺癌和前列腺癌中是有用的。还公开了含有这些化合物的药物组合物和治疗癌症的方法。
• Synthesis of Potent Oxindole CDK2 Inhibitors
  作者：Apos Dermatakis、Kin-Chun Luk、Wanda DePinto

  DOI：10.1016/s0968-0896(03)00036-1

  日期：2003.4

  A series of oxindole CDK2 inhibitors was synthesized. These novel analogues have a saturated monosubstituted cyclic moiety at their C-4 position that mimics the ribofuranoside of ATP. This substitution afforded agents with increased potency relative to the parent indolinone and nanomolar range IC50 against the CDK2 enzyme and two cancer cell lines. (C) 2003 Elsevier Science Ltd. All rights reserved.