2-amino-3-(5-methyl-1H-indol-3-yl)propan-1-ol | 913718-39-5

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吲哚及其衍生物
• 英文名称: 2-amino-3-(5-methyl-1H-indol-3-yl)propan-1-ol
• CAS: 913718-39-5
• 化学式: C₁₂H₁₆N₂O
• 分子量: 204.272
• InChiKey: OFKPYHCGHDVIJM-UHFFFAOYSA-N

物化性质

• 沸点：
  453.3±40.0 °C(Predicted)
• 密度：
  1.208±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  1.1
• 重原子数：
  15
• 可旋转键数：
  3
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.33
• 拓扑面积：
  62
• 氢给体数：
  3
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  2-amino-3-(5-methyl-1H-indol-3-yl)propan-1-ol 在 sodium ethanolate 、 三氟乙酸 作用下， 以 四氢呋喃 、 乙醇 为溶剂， 反应 5.0h， 生成
  参考文献：
  名称：

  Structure-activity relationship for DNA topoisomerase II-induced DNA cleavage by azatoxin analogues

  摘要：

  Eighteen analogues of the nonintercalative DNA topoisomerase II (topo II)-active epipodophyllotoxin-ellipticine hybrid, azatoxin, were synthesized and evaluated for their ability to induce topo II-mediated DNA strand breaks in vitro. In general, the SAR profile of the azatoxins showed more homology with that of the epipodophyllotoxins than with the ellipticines. Of the compounds studied, only fluoro substitution at the 8-, 9, and 10-positions of azatoxins enhanced activity, with 9-fluoroazatoxin being the most active compound in this series. (C) 1997 Elsevier Science Ltd.

  DOI：

  10.1016/s0968-0896(97)00113-2
• 作为产物：
  描述：

  5-甲基-DL-色氨酸 在 盐酸 、 sodium tetrahydroborate 作用下， 以 乙醇 、 水 为溶剂， 反应 6.0h， 生成 2-amino-3-(5-methyl-1H-indol-3-yl)propan-1-ol
  参考文献：
  名称：

  Structure-activity relationship for DNA topoisomerase II-induced DNA cleavage by azatoxin analogues

  摘要：

  Eighteen analogues of the nonintercalative DNA topoisomerase II (topo II)-active epipodophyllotoxin-ellipticine hybrid, azatoxin, were synthesized and evaluated for their ability to induce topo II-mediated DNA strand breaks in vitro. In general, the SAR profile of the azatoxins showed more homology with that of the epipodophyllotoxins than with the ellipticines. Of the compounds studied, only fluoro substitution at the 8-, 9, and 10-positions of azatoxins enhanced activity, with 9-fluoroazatoxin being the most active compound in this series. (C) 1997 Elsevier Science Ltd.

  DOI：

  10.1016/s0968-0896(97)00113-2

文献信息

• Acyltryptophanols
  申请人：Wortmann Lars

  公开号：US20070060573A1

  公开（公告）日：2007-03-15

  The present patent application relates to acyltryptophanols of the general formula I, in which Q, X, Y, W, R1, R2, R3, R4, R5, R8 have the meanings stated in the description. The compounds according to the invention are effective FSH antagonists and can be used for example for fertility control in men or in women, or for the prevention and/or treatment of osteoporosis.

  本专利申请涉及一般式I的酰基色氨酸醇，其中Q、X、Y、W、R1、R2、R3、R4、R5、R8具有说明书中所述的含义。本发明的化合物是有效的FSH拮抗剂，例如可用于男性或女性的生育控制，或用于骨质疏松症的预防和/或治疗。
• Fused Thiazole Derivatives as Kinase Inhibitors
  申请人：Alexander Rikki Peter

  公开号：US20080306060A1

  公开（公告）日：2008-12-11

  A series of 5,6-dihydro-1,3-benzothiazol-7(4H)-one derivatives, and analogues thereof, which are substituted in the 2-position by an optionally substituted morpholin-4-yl moiety, being selective inhibitors of PD kinase enzymes, are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, neurodegenerative, metabolic, oncological, nociceptive or ophthalmic conditions.

  一系列取代在2位位置具有可选取代的morpholin-4-yl基团的5,6-二氢-1,3-苯并噻唑-7(4H)-酮衍生物及其类似物，是选择性PD激酶酶抑制剂，在医学上具有益处，例如在治疗炎症、自身免疫、心血管、神经退行性、代谢、肿瘤、疼痛或眼科疾病方面。
• Synthesis of 6-substituted indolactams by microbial conversion
  作者：Kazuhiro Irie、Maya Iguchi、Tsuneyuki Oda、Yoko Suzuki、Shigenori Okuno、Hajime Ohigashi、Koichi Koshimizu、Hideo Hayashi、Motoo Arai、Hoyoku Nishino、Akio Iwashima

  DOI：10.1016/0040-4020(95)00298-m

  日期：1995.5

  New indolactam derivatives (24-27) with a fluorine, bromine, iodine or methyl group at position 6 of (-)-indolactam-V (1) were synthesized from corresponding seco-compounds (6-substituted N-methyl-L-valyl-L-tryptophanols) by the microbial conversion using Streptoverticilium blastmyceticum NA34-17. (-)-5-Fluoroindolactam-V (23) and (-)-7-methylindolactam-V (28) were similarly obtained by this method. (-)-6-Methylindolactam-V (27) had almost the same biological activities as (-)-7-methylindolactam-V (28), indicating that the substituent effect at position 6 of (-)-indolactam-V (1) is similar to that at position 7.
• FUSED THIAZOLE DERIVATIVES AS KINASE INHIBITORS
  申请人：UCB Pharma, S.A.

  公开号：EP1881827B1

  公开（公告）日：2011-09-28
• US7888344B2
  申请人：——

  公开号：US7888344B2

  公开（公告）日：2011-02-15