5-(naphthalen-2-yl)-5,6,7,8-tetrahydroimidazo[1,5-a]pyridine | 129234-39-5

• 分子结构分类: 有机化合物 - 有机杂环化合物
• 英文名称: 5-(naphthalen-2-yl)-5,6,7,8-tetrahydroimidazo[1,5-a]pyridine
• 英文别名: 5-(2-naphthyl)-5,6,7,8-tetrahydroimidazo[1,5-a]pyridine；5-Naphthalen-2-yl-5,6,7,8-tetrahydroimidazo[1,5-a]pyridine
• CAS: 129234-39-5
• 化学式: C₁₇H₁₆N₂
• 分子量: 248.327
• InChiKey: CYVOOOCLVNNILU-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.7
• 重原子数：
  19
• 可旋转键数：
  1
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.24
• 拓扑面积：
  17.8
• 氢给体数：
  0
• 氢受体数：
  1

反应信息

• 作为产物：
  描述：

  对甲基苯磺酰甲基异腈 、 2-(naphthalen-2-yl)piperidine 在 正丁基锂 、 2,2,2-三氟苯乙酮 、 叔丁胺 作用下， 以 乙醚 、 正己烷 、 甲醇 为溶剂， 以60%的产率得到5-(naphthalen-2-yl)-5,6,7,8-tetrahydroimidazo[1,5-a]pyridine
  参考文献：
  名称：

  通过脂环胺的 α-C–H/N–H 环化合成多环咪唑

  摘要：

  脂环族仲胺通过一个简单的程序转化为相应的环稠合咪唑，该程序包括氧化亚胺形成，然后进行范洛森反应。具有现有 α-取代基的胺在 α'-位进行区域选择性环融合。该方法用于法屈唑的合成。

  DOI：

  10.1055/a-2022-1511

文献信息

• Substituted 5,6,7,8-tetrahydroimidazo[1,5-a]pyridines and process for their preparation
  申请人：FARMITALIA CARLO ERBA S.r.l.

  公开号：EP0356673A2

  公开（公告）日：1990-03-07

  Object of the invention are 5,6,7,8-tetrahydroimidazo [1.5-a] pyridines having the following formula (I) wherein W is a) a 2-naphthyl or 1- or 2- or 9-anthryl radical wherein each benzene ring is unsubstituted or substituted by a substituent chosen from (a₁)halogen, C₁-C₄ alkyl, aryl, aryl-C₁-C₄ alkyl, hydroxy, C₁-C₄ alkoxy aryloxy, aryl-C₁-C₄ alkoxy, formyloxy, C₂-C₅ alkanoyloxy, aroyloxy, mercapto,C₁-C₄ alkylthio, arylthio, aryl-C₁-C₄ alkylthio, C₁-C₄ alkylsulfonyl,arylsulfonyl, C₂-C₅ alkanoyl­thio, C₂-C₅ alkanoylamino, aroylamino, C₂-C₅ alkanoyl, aroyl,car­boxy, C₂-C₅ alkoxycarbonyl, cyano, nitro, mono- or di-(C₁-C₄ alkyl) carbamyl, amino and mono- (C₁-C₄ alkyl) amino (a₂) di-(C₁-C₄ alkyl) amino, morpholino, piperazino and C₁-C₄ alkyl-­-N-substituted piperazino, and (a₃) a quaternary ammonium radical which is a radical as defined above under (a₂) having a or a further C₁-C₄ alkyl group as the fourth substituent on the nitrogen atom; or b) a pyridyl, pyrazinyl , pyrimidyl or pyridazinyl ring wherein each said ring is unsubstituted or substituted by a substituent chosen from (a₁) to (a₃) above; and the pharma­ceutically acceptable salts thereof, which are aromatase inhibitors.

  本发明的目的是具有下式（I）的 5、6、7、8-四氢咪唑并[1.5-a]吡啶 其中 W 是 a) 2-萘基或 1-或 2-或 9-蒽基，其中每个苯环未被取代或被选自以下的取代基取代 (a₁)halogen, C₁-C₄ alkyl, aryl, aryl-C₁-C₄ alkyl, hydroxy, C₁-C₄ alkoxy aryloxy, aryl-C₁-C₄ alkoxy, formyloxy、C₂-C₅烷氧基、芳氧基、巯基、C₁-C₄烷硫基、芳基硫基、芳基-C₁-C₄烷硫基、C₁-C₄烷基磺酰基、芳基磺酰基、C₁-C₄烷基磺酰基C₂-C₅烷酰硫基，C₂-C₅烷酰氨基，芳基氨基，C₂-C₅烷酰基，芳基，羧基、C₂-C₅烷氧羰基、氰基、硝基、单-或二-(C₁-C₄烷基)羰基、氨基和单-(C₁-C₄烷基)氨基 (a₂) 二(C₁-₄烷基)氨基、吗啉基、哌嗪基和 C₁-C₄ 烷基--N-取代的哌嗪基，以及 (a₃) 季铵基，该季铵基是上文(a₂)中定义的基团，其氮原子上的第四个取代基是一个或另一个 C₁-C₄ 烷基；或 b) 吡啶基、吡嗪基、嘧啶基或哒嗪基环，其中每个所述环未被取代或被选自上述 (a₁) 至 (a₃) 的取代基取代；及其药学上可接受的盐，它们是芳香化酶抑制剂。
• Aromatase inhibition to enhance assisted reproduction
  申请人：ARES TRADING S.A.

  公开号：EP1759734A2

  公开（公告）日：2007-03-07

  The use of at least one aromatase inhibitor in the production of a medicament for improving the implantation and pregnancy rates for a female undergoing assisted reproduction treatment, which comprises one or more daily doses of an aromatase inhibitor (Al) for administration during assisted reproduction cycles or ovarian stimulation cycles, wherein the doses of AI are selected from amounts effective to reduce serum estradiol levels. Also disclosed are related pharmaceutical preparations and packages.

  使用至少一种芳香化酶抑制剂生产一种药物，用于提高接受辅助生殖治疗的女性的着床率和妊娠率，该药物包括一种或多种每日剂量的芳香化酶抑制剂（Al），用于在辅助生殖周期或卵巢刺激周期期间给药，其中AI的剂量选自有效降低血清雌二醇水平的量。还公开了相关的药物制剂和包装。
• Single dose aromatase inhibitor for treating infertility
  申请人：——

  公开号：US20040171660A1

  公开（公告）日：2004-09-02

  The use of an aromatase inhibitor (AI) in the preparation of a medicament for use in inducing ovulation in a female suffering from anovulatory infertility which comprises administering to said female a single dose of the at least one aromatase inhibitor. The use of an aromatase inhibitor (AI) for the preparation of a medicament comprising a single dose of at least one aromatase inhibitor (AI) for administration to an ovulating female suffering from unexplained infertility or other types of ovulatory infertility early in one or more menstrual cycles. Such a medicament may also be administered to an anovulatory female in combination with a plurality of daily doses of follicle stimulating hormone (FSH) whereby the dosage levels of FSH may be reduced. The use of AI in the preparation of a medicament for administration to a female who is a poor responder to FSH, which comprises a combination of a single dose of AI with a plurality of daily doses of FSH is also disclosed. The related pharmaceutical preparations and packages are also described.

  芳香化酶抑制剂(AI)在制备用于诱导患有无排卵性不孕症的女性排卵的药物中的用途，包括向所述女性施用单剂量的至少一种芳香化酶抑制剂。芳香化酶抑制剂(AI)的用途，用于制备一种包含单剂量至少一种芳香化酶抑制剂(AI)的药剂，给患有不明原因不孕症或其他类型排卵性不孕症的排卵期女性在一个或多个月经周期的早期给药。这种药物也可与多种每日剂量的促卵泡激素（FSH）联合用于无排卵女性，从而降低促卵泡激素的剂量水平。此外，还公开了 AI 在制备用于对 FSH 反应不佳的女性的药物中的用途，该药物包括单剂量 AI 与多剂量每日 FSH 的组合。还描述了相关的药物制剂和包装。
• Multiple dose aromatase inhibitor for treating infertility
  申请人：——

  公开号：US20040235804A1

  公开（公告）日：2004-11-25

  A method of inducing ovulation in a female suffering from anovulatory infertility which comprises administering to said female two or more daily doses of at least one aromatase inhibitor. A method for augmenting ovulation in an ovulating female suffering from unexplained infertility or another type of ovulatory infertility which comprises administering to said female two or more daily doses of at least one aromatase inhibitor early in one or more menstrual cycles. A method of substantially reducing dosage levels of follicle stimulating hormone (FSH) for administration to a female undergoing infertility treatment which comprises administering a combination of two or more daily doses of at least one aromatase inhibitor (AI) with a plurality of daily doses of follicle stimulating hormone (FSH). A method of increasing response to a follicle stimulating hormone from a female who is a poor responder to follicle stimulation, which comprises administering a combination of two or more daily doses or at least one aromatase inhibitor (AI) with a plurality of daily doses of follicle stimulating hormone (FSH). Also disclosed are related pharmaceutical preparations and uses.

  一种诱导无排卵性不孕症女性排卵的方法，包括向所述女性施用两种或两种以上每日剂量的至少一种芳香化酶抑制剂。一种促进患有不明原因不孕症或另一种排卵性不孕症的女性排卵的方法，包括在一个或多个月经周期的早期给所述女性服用两个或多个每日剂量的至少一种芳香化酶抑制剂。一种大幅降低促卵泡激素(FSH)剂量水平的方法，用于对接受不孕治疗的女性用药，该方法包括将两种或两种以上日剂量的至少一种芳香化酶抑制剂(AI)与多种日剂量的促卵泡激素(FSH)联合用药。一种增加对卵泡刺激反应差的女性对卵泡刺激激素的反应的方法，它包括给药两种或两种以上每日剂量或至少一种芳香化酶抑制剂（AI）与多种每日剂量的卵泡刺激激素（FSH）的组合。还公开了相关的药物制剂和用途。
• Pharmaceutical composition comprisng an aromatase inhibitor and an estrogen suitable for hormone replacement therapy for a male
  申请人：——

  公开号：US20040235812A1

  公开（公告）日：2004-11-25

  A pharmaceutical preparation for males for increasing physiologic endogenous testosterone comprising at least one aromatase inhbitor and an estrogen and methods of use thereof for increasing male libido are provided.

  本研究提供了一种用于增加男性生理性内源性睾酮的药物制剂，该制剂包含至少一种芳香化酶抑制剂和一种雌激素，并提供了增加男性性欲的使用方法。