Tert-butyl 6-formyl-5-azaspiro[2.4]heptane-5-carboxylate | 1613292-77-5

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡咯烷类
• 英文名称: Tert-butyl 6-formyl-5-azaspiro[2.4]heptane-5-carboxylate
• 英文别名: tert-butyl 6-formyl-5-azaspiro[2.4]heptane-5-carboxylate
• CAS: 1613292-77-5
• 化学式: C₁₂H₁₉NO₃
• 分子量: 225.288
• InChiKey: FLLMFXSFFYGQFI-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.4
• 重原子数：
  16
• 可旋转键数：
  3
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.83
• 拓扑面积：
  46.6
• 氢给体数：
  0
• 氢受体数：
  3

反应信息

• 作为产物：
  描述：

  tert-butyl 5-azaspiro[2.4]heptane-5-carboxylate 、 N,N-二甲基甲酰胺 在 仲丁基锂 作用下， 以 四氢呋喃 、 环己烷 为溶剂， 反应 0.59h， 生成 tert-butyl 4-formyl-5-azaspiro[2.4]heptane-5-carboxylate 、 Tert-butyl 6-formyl-5-azaspiro[2.4]heptane-5-carboxylate
  参考文献：
  名称：

  [EN] PYRIDINE-2-AMIDES USEFUL AS CB2 AGONISTS
  [FR] PYRIDINE-2-AMIDES UTILES COMME AGONISTES DE CB2

  摘要：

  这项发明涉及到公式（I）中的CB2激动剂，其中R1至R4的定义如描述和索赔中所述。公式（I）的化合物可用作药物。

  公开号：

  WO2014086806A1

文献信息

• [EN] SPIRO AMINO COMPOUNDS SUITABLE FOR THE TREATMENT OF INTER ALIA SLEEP DISORDERS AND DRUG ADDICTION<br/>[FR] COMPOSÉS SPIRO-AMINIQUES CONVENANT AU TRAITEMENT, NOTAMMENT, DES TROUBLES DU SOMMEIL ET DE LA PHARMACODÉPENDANCE
  申请人：ROTTAPHARM SPA

  公开号：WO2011006960A1

  公开（公告）日：2011-01-20

  The invention concerns a spiro-amino compound of Formula (Vl) wherein m is 1 or 2 or 3, n is 1 or 2, R is selected from a 5- or 6-membered aromatic ring and a 5- or 6-membered heteroaromatic ring comprising 1 to 3 heteroatoms selected from S, O e N, such ring being substituted with one or two substituents selected from the group consisting of (C1-C3)alkyl, halogen, (C3-C5)cycloalkyloxy, (C1-C3)alkylcarbonyl, phenyl optionally substituted with one or more halogen atoms, a 5- or 6-membered heterocycle comprising at least one nitrogen atom; P is a substituent Q or COQ, wherein Q is selected from the group consisting of phenyl, pyridil, pyrimidil, quinolyl, isoquinolyl, quinoxalyl, benzofuranyl, imidazotriazolyl, being such Q optionally substituted with one or more substituents selected from the group consisting of (C1-C3)alkyl, halogen, trifluoromethyl, carbammido, methylcarbammido, carboxy, methylcarboxy or a pharmaceutically acceptable salt thereof.

  本发明涉及一种式(Vl)的螺环氨基化合物，其中m为1或2或3，n为1或2，R选自5-或6-成环的芳香环和5-或6-成环的杂芳香环，包含1至3个选自S、O和N的杂原子，该环被1个或2个选自(C1-C3)烷基、卤素、(C3-C5)环烷基氧基、(C1-C3)烷基羰基、可选地用1个或多个卤素原子取代的苯基、至少含有一个氮原子的5-或6-成环杂环所取代；P是取代基Q或COQ，其中Q选自苯基、吡啶基、嘧啶基、喹啉基、异喹啉基、喹喔啉基、苯并呋喃基、咪唑三唑基，该Q可选项地被1个或多个选自(C1-C3)烷基、卤素、三氟甲基、碳酰胺、甲基碳酰胺、羧基、甲基羧基的取代基所取代，或其药用可接受盐。
• Spiro amino compounds suitable for the treatment of inter alia sleep disorders and drug addiction
  申请人：Rottapharm S.p.A.

  公开号：EP2275421A1

  公开（公告）日：2011-01-19

  The invention concerns a spiro-amino compound of Formula (VI) wherein m is 1 or 2 or 3, n is 1 or 2, R is selected from a 5- or 6-membered aromatic ring and a 5-or 6-membered heteroaromatic ring comprising 1 to 3 heteroatoms selected from S, O e N, such ring being substituted with one or two substituents selected from the group consisting of (C1-C3)alkyl, (C3-C5)cycloalkyloxy, (C1-C3)alkylcarbonyl, phenyl optionally substituted with one or more halogen atoms, a 5- or 6-membered heterocycle comprising at least one nitrogen atom; P is a substituent Q or COQ, wherein Q is selected from the group consisting of phenyl, pyridil, pyrimidil, quinolyl, isoquinolyl, quinoxalyl, benzofuranyl, imidazotriazolyl, being such Q optionally substituted with one or more substituents selected from the group consisting of (C1-C3)alkyl, halogen, trifluoromethyl, carbammido, methylcarbammido, carboxy.

  该发明涉及式（VI）的螺环氨基化合物，其中m为1或2或3，n为1或2，R选自含有5或6个成员的芳香环和含有1至3个来自S、O和N的杂原子的5或6个成员杂原子环，该环被一个或两个取代基所取代，所述取代基选自（C1-C3）烷基，（C3-C5）环烷氧基，（C1-C3）烷基羰基，苯基（可选地取代一个或多个卤素原子），含有至少一个氮原子的5或6个成员杂环；P为取代基Q或COQ，其中Q选自苯基，吡啶基，嘧啶基，喹啉基，异喹啉基，喹啉基，苯并呋喃基，咪唑三唑基，该Q可选地被一个或多个取代基所取代，所述取代基选自（C1-C3）烷基，卤素，三氟甲基，氨基甲酰基，甲基氨基甲酰基，羧基。
• SPIRO AMINO COMPOUNDS SUITABLE FOR THE TREATMENT OF INTER ALIA SLEEP DISORDERS AND DRUG ADDICTION
  申请人：Stasi Luigi Piero

  公开号：US20120115882A1

  公开（公告）日：2012-05-10

  A spiro-amino compound of Formula (VI) wherein m is 1 or 2 or 3, n is 1 or 2, R is selected from a 5- or 6-membered aromatic ring and a 5- or 6-membered heteroaromatic ring comprising 1 to 3 heteroatoms selected from S, O and N, such ring being substituted with one or two substituents selected from the group consisting of (C 1 -C 3 )alkyl, halogen, (C 3 -C 5 )cycloalkyloxy, (C 1 -C 3 )alkylcarbonyl, phenyl optionally substituted with one or more halogen atoms, a 5- or 6-membered heterocycle comprising at least one nitrogen atom; P is a substituent Q or COQ, wherein Q is selected from the group consisting of phenyl, pyridyl, pyrimidyl, quinolyl, isoquinolyl, quinoxalyl, benzofuranyl, imidazotriazolyl, being such Q optionally substituted with one or more substituents selected from the group consisting of (C 1 -C 3 )alkyl, halogen, trifluoromethyl, carbammido, methylcarbammido, carboxy, methylcarboxy or a pharmaceutically acceptable salt thereof.

  式（VI）的螺环氨基化合物，其中m为1或2或3，n为1或2，R从5或6成员芳香环和5或6成员杂芳香环中选择，该环包含1到3个从S，O和N中选择的杂原子，该环被1或2个取代基所取代，所述取代基选择自(C1-C3)烷基，卤素，(C3-C5)环烷氧基，(C1-C3)烷基羰基，苯基，该苯基可选择一个或多个卤素原子进行取代，以及一种包含至少一个氮原子的5或6成员杂环；P是取代基Q或COQ，其中Q从苯基，吡啶基，嘧啶基，喹啉基，异喹啉基，喹嗪基，苯并呋喃基，咪唑三唑基中选择，所述Q可选择一个或多个取代基进行取代，所述取代基选择自(C1-C3)烷基，卤素，三氟甲基，氨基甲酰基，甲基氨基甲酰基，羧基，甲基羧基或其药学上可接受的盐。
• PYRIDINE-2-AMIDES USEFUL AS CB2 AGONISTS
  申请人：HOFFMANN-LA ROCHE INC.

  公开号：US20150299165A1

  公开（公告）日：2015-10-22

  The invention relates to CB2 agonists of formula (I) wherein R 1 to R 4 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.

  本发明涉及公式（I）中R1到R4如说明书和权利要求书中所定义的CB2激动剂。公式（I）的化合物可用作药物。
• LIGAND-CYTOTOXICITY DRUG CONJUGATE, PREPARING METHOD THEREFOR, AND APPLICATION THEREOF
  申请人：Jiangsu Hengrui Medicine Co. Ltd.

  公开号：EP3251698A1

  公开（公告）日：2017-12-06

  Provide are a ligand-cytotoxicity drug conjugate with a general formula of PC-L-Dr, a preparing method thereof, and applications of the ligand-cytotoxicity drug conjugate and pharmaceutical compositions comprising the same in preparing drugs for treating cancers by means of receptor regulation.

  提供一种通式为 PC-L-Dr 的配体-毒性药物共轭物及其制备方法，以及该配体-毒性药物共轭物和包含该配体-毒性药物共轭物的药物组合物在制备通过受体调节治疗癌症的药物中的应用。