ethyl 5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-3-aminonaphthalene-2-carboxylate | 191469-46-2

• 分子结构分类: 有机化合物 - 苯类化合物 - 萘
• 英文名称: ethyl 5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-3-aminonaphthalene-2-carboxylate
• 英文别名: ethyl-3-amino-5,5,8,8-tetrahydro-5,5,8,8-tetramethylnaphtalene-2-carboxylate；ethyl 3-amino-5,5,8,8-tetramethyl-6,7-dihydronaphthalene-2-carboxylate
• CAS: 191469-46-2
• 化学式: C₁₇H₂₅NO₂
• 分子量: 275.391
• InChiKey: NWYIWVNRQQJKRU-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  5.1
• 重原子数：
  20
• 可旋转键数：
  3
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.59
• 拓扑面积：
  52.3
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  ethyl 5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-3-aminonaphthalene-2-carboxylate 在 溴 作用下， 以 溶剂黄146 为溶剂， 以79.5%的产率得到ethyl 2-Amino-1-bromo-5,5,8,8-tetrahydro-5,5,8,8-tetramethylnaphthalene-3-carboxylate
  参考文献：
  名称：

  Aryl or heteroaryl amides of tetrahydronaphthalene, chroman, thiochroman

  摘要：

  式##STR1##中的化合物具有类似于视黄醇的生物活性，其中符号的含义在说明书中定义。

  公开号：

  US05675024A1
• 作为产物：
  描述：

  ethyl-3-nitro-5,5,8,8-tetrahydro-5,5,8,8-tetramethylnaphtalene-2-carboxylate 在 盐酸 、 titanium(III) chloride 作用下， 以 四氢呋喃 、 溶剂黄146 为溶剂， 生成 ethyl 5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-3-aminonaphthalene-2-carboxylate
  参考文献：
  名称：

  Aryl or heteroaryl amides of tetrahydronaphthalene, chroman, thichroman and 1,2,3,4-tetrahydroquinolinecarboxlic acids, having an electron withdrawing substituent in the aromatic or heteroaromatic moiety, having retinoid-like biological activity

  摘要：

  该式化合物具有类视黄醇生物活性，其中符号的含义在规范中定义。

  公开号：

  US06342602B1

文献信息

• Methods of treatment with compounds having RAR.sub..alpha. receptor
  申请人：Allergan Sales, Inc.

  公开号：US05965606A1

  公开（公告）日：1999-10-12

  Retinoid compounds which act specifically or selectively on RAR.sub..alpha. receptor subtypes in preference over RAR.sub..beta. and RAR.sub..gamma. receptor subtypes, posses desirable pharmaceutical properties associated with retinoids, and are particularly suitable for treatment of tumors, such as acute monocytic leukemia, cervical carcinoma, myeloma, ovarian carcinomas and head and neck carcinomas, without having one or more undesirable side effects of retinoids, such as inducement of weight loss, mucocutaneous toxicity, skin irritation and teratogenecity.

  对RAR.sub..alpha.受体亚型具有特异性或选择性作用，优先于RAR.sub..beta.和RAR.sub..gamma.受体亚型的视黄醇类化合物具有与视黄醇相关的理想药理特性，并特别适用于治疗肿瘤，如急性单核细胞白血病、宫颈癌、骨髓瘤、卵巢癌和头颈癌，而不会产生视黄醇的一个或多个不良副作用，如诱导体重减轻、粘膜皮肤毒性、皮肤刺激和致畸性。
• Methods of treatment with compounds having RAR alpha receptor specific or selective activity
  申请人：Allergan Sales, Inc.

  公开号：US20020077360A1

  公开（公告）日：2002-06-20

  Retinoid compounds which act specifically or selectively on RAR &agr; receptor subtypes in preference over RAR &bgr; and RAR &Ggr; receptor subtypes, posses desirable pharmaceutical properties associated with retinoids, and are particularly suitable for treatment of tumors, such as acute monocytic leukemia, cervical carcinoma, myeloma, ovarian carcinomas and head and neck carcinomas, without having one or more undesirable side effects of retinoids, such as inducement of weight loss, mucocutaneous toxicity, skin irritation and teratogenecity.

  作用于RARα亚型的视黄酸类化合物，具有优于RARβ和RARγ亚型的选择性或特异性，具有与视黄酸相关的理想药物特性，特别适用于治疗肿瘤，如急性单核细胞白血病、宫颈癌、骨髓瘤、卵巢癌和头颈癌，而不具有视黄酸的一个或多个不良副作用，如诱导体重减轻、粘膜皮肤毒性、皮肤刺激和致畸性。
• Methods of treatment with compounds having RAR&agr; receptor specific or selective activity
  申请人：Allergan, Inc.

  公开号：US06610744B2

  公开（公告）日：2003-08-26

  Retinoid compounds which act specifically or selectively on RAR&agr; receptor subtypes in preference over RAR&bgr; and RAR&Ggr; receptor subtypes, posses desirable pharmaceutical properties associated with retinoids, and are particularly suitable for treatment of tumors, such as acute monocytic leukemia, cervical carcinoma, myeloma, ovarian carcinomas and head and neck carcinomas, without having one or more undesirable side effects of retinoids, such as inducement of weight loss, mucocutaneous toxicity, skin irritation and teratogenecity.

  对RARα受体亚型具有特异性或选择性作用，而优先于RARβ和RARγ受体亚型的视黄酸类化合物具有与视黄酸相关的理想药物特性，特别适用于治疗肿瘤，例如急性单核细胞白血病、宫颈癌、骨髓瘤、卵巢癌和头颈癌，而不具有视黄酸的一个或多个不良副作用，例如诱导体重减轻、粘膜皮肤毒性、皮肤刺激和致畸性。
• METHODS OF TREATMENT WITH COMPOUNDS HAVING RAR $g(a)? RECEPTOR SPECIFIC OR SELECTIVE ACTIVITY
  申请人：Vision Pharmaceuticals L.P.

  公开号：EP0869782A2

  公开（公告）日：1998-10-14
• ARYL OR HETEROARYL AMIDES OF TETRAHYDRONAPHTHALENE, CHROMAN, THIOCHROMAN AND 1,2,3,4-TETRAHYDROQUINOLINE CARBOXYLIC ACIDS HAVING RETINOID-LIKE BIOLOGICAL ACTIVITY
  申请人：Allergan Sales, Inc.

  公开号：EP0876330B1

  公开（公告）日：2001-03-28