1-methoxy-4-fluoro-5-iodo-2-methylbenzene | 741716-19-8

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯酚醚
• 英文名称: 1-methoxy-4-fluoro-5-iodo-2-methylbenzene
• 英文别名: 1-Fluoro-2-iodo-4-methoxy-5-methylbenzene
• CAS: 741716-19-8
• 化学式: C₈H₈FIO
• 分子量: 266.054
• InChiKey: BSCRXLNFUWALFO-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3
• 重原子数：
  11
• 可旋转键数：
  1
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.25
• 拓扑面积：
  9.2
• 氢给体数：
  0
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  4-氨基-2-(乙基硫代)-N-甲氧基-N-甲基-5-嘧啶羧酰胺 、 1-methoxy-4-fluoro-5-iodo-2-methylbenzene 以to give (4-amino-2-ethylsulfanyl-pyrimidin-5-yl)-(2-fluoro-5-methoxy-4-methyl-phenyl)-methanone的产率得到(4-Amino-2-ethylsulfanyl-pyrimidin-5-yl)-(2-fluoro-5-methoxy-4-methyl-phenyl)-methanone
  参考文献：
  名称：

  4-aminopyrimidine-5-one derivatives

  摘要：

  揭示了新型中间化合物。这些化合物在合成4-氨基嘧啶-5-酮衍生物中非常有用，这些衍生物抑制细胞周期依赖性激酶，特别是细胞周期依赖性激酶4（Cdk4）。4-氨基嘧啶-5-酮衍生物及其药学上可接受的盐具有抗增殖活性，并且在治疗或控制癌症，特别是实体肿瘤方面非常有用。

  公开号：

  US20060229330A1
• 作为产物：
  描述：

  4-Fluoro-5-iodo-2-methylphenol 、 碘甲烷 在 potassium carbonate 作用下， 以 丙酮 为溶剂， 反应 3.0h， 以70%的产率得到1-methoxy-4-fluoro-5-iodo-2-methylbenzene
  参考文献：
  名称：

  WO2006/76246

  摘要：

  公开号：

文献信息

• Phenylglycinamide derivatives useful as anticoagulants
  申请人：Zhang Xiaojun

  公开号：US20060166997A1

  公开（公告）日：2006-07-27

  The present invention relates generally to phenylglycinamide derivatives that inhibit serine proteases. In particular it is directed to novel phenylglycinamide derivatives, and analogues thereof, which are useful as selective inhibitors of serine protease enzymes of the coagulation cascade; for example thrombin, factor VIIa, factor Xa, factor XIa, factor IXa, and/or plasma kallikrein. In particular, it relates to compounds that are factor VIIa inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of using the same.

  本发明一般涉及抑制丝氨酸蛋白酶的苯基甘氨酰衍生物。具体而言，本发明涉及新型苯基甘氨酰衍生物及其类似物，其可用作凝血级联反应的丝氨酸蛋白酶酶的选择性抑制剂；例如凝血酶、第VIIa因子、第Xa因子、第XIa因子、第IXa因子和/或血浆激肽。特别是，它涉及到的化合物是第VIIa因子的抑制剂。本发明还涉及包含这些化合物的制药组合物及其使用方法。
• 4-Aminopyrimidine-5-one derivatives
  申请人：Hoffmann-La Roche Inc.

  公开号：US07157455B2

  公开（公告）日：2007-01-02

  Novel 4-aminopyrimidine-5-one derivatives are disclosed. These compounds inhibit cyclin-dependent kinases, in particular cyclin-dependent kinase 4 (Cdk4). These compounds and their pharmaceutically acceptable salts and esters have antiproliferative activity and are useful in the treatment or control of cancer, in particular solid tumors. This invention is also directed to pharmaceutical compositions containing such compounds and to methods of treating or controlling cancer, most particularly the treatment or control of breast, lung, colon and prostate tumors. Also disclosed are intermediates useful in the preparation of these novel 4-aminopyrimidine-5-one derivatives.

  本发明披露了新型4-氨基嘧啶-5-酮衍生物。这些化合物抑制细胞周期依赖性激酶，特别是细胞周期依赖性激酶4（Cdk4）。这些化合物及其药学上可接受的盐和酯具有抗增殖活性，并且在治疗或控制癌症，特别是实体瘤方面非常有用。本发明还涉及含有这些化合物的制药组合物以及治疗或控制癌症的方法，特别是乳腺癌、肺癌、结肠癌和前列腺癌的治疗或控制方法。还披露了在制备这些新型4-氨基嘧啶-5-酮衍生物过程中有用的中间体。
• IMPORT OF UNNATURAL OR MODIFIED NUCLEOSIDE TRIPHOSPHATES INTO CELLS VIA NUCLEIC ACID TRIPHOSPHATE TRANSPORTERS
  申请人：The Scripps Research Institute

  公开号：EP3943607A1

  公开（公告）日：2022-01-26

  A recombinantly expressed nucleotide triphosphate transporter efficiently imports the triphosphates of unnatural nucleotides into cells, and the endogenous cellular machinery incorporates those nucleotides into cellular nucleic acids. UBPs can therefore form within the cell's nucleic acids. Moreover, neither the presence of the unnatural triphosphates nor the replication of the UBP represents a significant growth burden. The UBP is not efficiently excised by nucleic acid repair pathways, and therefore can be retained as long as the unnatural triphosphates are available in the growth medium. Thus, the resulting cell is the first organism to stably propagate an expanded genetic alphabet.

  重组表达的核苷酸三磷酸转运体能有效地将非天然核苷酸的三磷酸酯导入细胞，而内源性细胞机制则会将这些核苷酸整合到细胞核酸中。因此，细胞核酸中会形成 UBPs。此外，非天然三磷酸酯的存在和 UBP 的复制都不会对生长造成重大负担。核酸修复途径不能有效地清除 UBP，因此只要生长培养基中存在非天然三磷酸盐，UBP 就能保留下来。因此，由此产生的细胞是第一个稳定繁殖扩增遗传字母的生物体。
• Import of unnatural or modified nucleoside triphosphates into cells via nucleic acid triphosphate transporters
  申请人：The Scripps Research Institute

  公开号：US10513706B2

  公开（公告）日：2019-12-24

  A recombinantly expressed nucleotide triphosphate transporter efficiently imports the triphosphates of unnatural nucleotides into cells, and the endogenous cellular machinery incorporates those nucleotides into cellular nucleic acids. UBPs can therefore form within the cell's nucleic acids. Moreover, neither the presence of the unnatural triphosphates nor the replication of the UBP represents a significant growth burden. The UBP is not efficiently excised by nucleic acid repair pathways, and therefore can be retained as long as the unnatural triphosphates are available in the growth medium. Thus, the resulting cell is the first organism to stably propagate an expanded genetic alphabet.

  重组表达的核苷酸三磷酸转运体能有效地将非天然核苷酸的三磷酸酯导入细胞，而内源性细胞机制则会将这些核苷酸整合到细胞核酸中。因此，细胞核酸中会形成 UBPs。此外，非天然三磷酸酯的存在和 UBP 的复制都不会对生长造成重大负担。核酸修复途径不能有效地清除 UBP，因此只要生长培养基中存在非天然三磷酸盐，UBP 就能保留下来。因此，由此产生的细胞是第一个稳定繁殖扩增遗传字母的生物体。
• 4-AMINOPYRIMIDINE-5-ONE
  申请人：F.HOFFMANN-LA ROCHE AG

  公开号：EP1628619A2

  公开（公告）日：2006-03-01