4-(3-甲氧基-苯基)-1-甲基-哌啶 | 106275-88-1

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 哌啶类
• 中文名称: 4-(3-甲氧基-苯基)-1-甲基-哌啶
• 英文名称: 4-(3-methoxy-phenyl)-1-methyl-piperidine
• 英文别名: 4-(3-Methoxy-phenyl)-1-methyl-piperidin；4-(3-Methoxyphenyl)-1-methylpiperidine
• CAS: 106275-88-1
• 化学式: C₁₃H₁₉NO
• 分子量: 205.3
• InChiKey: TYSWSYPHKOIZFM-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.5
• 重原子数：
  15
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.54
• 拓扑面积：
  12.5
• 氢给体数：
  0
• 氢受体数：
  2

反应信息

• 作为产物：
  描述：

  3-(3-methoxy-phenyl)-glutaric acid dimethyl ester 在 lithium aluminium tetrahydride 、 乙醚 作用下， 生成 4-(3-甲氧基-苯基)-1-甲基-哌啶
  参考文献：
  名称：

  Piperidine Derivatives. XXX. 1,4-Dialkyl-4-arylpiperidines

  摘要：

  DOI：

  10.1021/ja01548a030

文献信息

• Direct Aminoalkylation of Arenes and Hetarenes via Ni-Catalyzed Negishi Cross-Coupling Reactions
  作者：Laurin Melzig、Andrey Gavryushin、Paul Knochel

  DOI：10.1021/ol702499h

  日期：2007.12.1

  room-temperature Ni-catalyzed cross-coupling of aminoalkylzinc halides, readily available from the corresponding aminoalkyl chlorides via Grignard reagents, with aryl and hetaryl electrophiles, allows a convenient one-step preparation of aminoalkyl (het)arenes, bearing a basic tertiary nitrogen in the side chain, including piperidine and tropane derivatives. Such aminoalkylarene scaffolds are widely present in

  氨基烷基锌卤化物的直接室温Ni催化交叉偶联很容易从相应的氨基烷基氯化物通过Grignard试剂与芳基和杂芳基亲电试剂获得，可以方便地一步制备带有碱性叔胺的氨基烷基（杂）芳烃侧链中的氮包括哌啶和托烷衍生物。这种氨基烷基亚芳基支架广泛存在于各种生物活性分子中。
• MODIFIED PYRIMIDINE GLUCOCORTICOID RECEPTOR MODULATORS
  申请人：Clark Robin D.

  公开号：US20090275600A1

  公开（公告）日：2009-11-05

  The present invention provides a novel class of modified pyrimidine compounds and compositions and methods of using the compounds as glucocorticoid receptor modulators.

  本发明提供了一种新型的改性嘧啶化合物类、组成物和使用该化合物作为糖皮质激素受体调节剂的方法。
• Modulators of CB1 Receptors
  申请人：Cooper Martin

  公开号：US20100144701A1

  公开（公告）日：2010-06-10

  Compounds of formula (I) suppress the normal signalling activity CB1 receptors, and are thus useful in the treatment of diseases or conditions which are mediated by CB1 receptor signalling activity, such as treatment of obesity and overweight, prevention of weigh gain, treatment of diseases and conditions directly or indirectly associated with obesity and overweight: wherein A 1 is hydrogen, —COOH,or tetrazolyl; p and q are independently 0 or 1; A3 is phenyl or cycloalkyl, either of which is optionally substituted with R 4 and/or R 5 ; R 4 and R 5 are independently —R 9 , —CN, —F, —Cl, —Br, —OR 9 , —NR 7 R 8 , —NR 7 COR 6 , —NR 7 SO 2 R 6 , —COR 6 , —SR 9 , —SOR 9 , or —SO 2 R 6 ; R 6 is C 1 -C 4 alkyl, cycloalkyl, —CF 3 or —NR 7 R 8 ; R 7 and R 8 are independently hydrogen, C 1 -C 4 alkyl or cycloalkyl; R 9 is hydrogen, C 1 -C 4 alkyl, C 1 -C 4 alkoxy, C 1 -C 4 alkoxy(C 1 -C 4 alkyl)-, cycloalkyl, or fully or partially fluorinated C 1 -C 4 alkyl; R 1 (i) a bond; (ii) a divalent radical of formula —(CH 2 ) a B 1 (CH 2 ) b wherein a and b are independently O, 1, 2 or 3 provided that a+b is 1, 2 or 3, and B 1 is —CO—, —O—, —S—, —SO—, —SO 2 —, —CH 2 —, —CHCH 3 —, —CHOH— or —NR 7 —; or (iii) a divalent radical selected from —C(R 10 )(R 11 )—*, —C(R 10 )(R 11 )—O—*, —C(R 10 )(R 11 )CH 2 —*, —C(R 10 )(R 11 )CH 2 —O—*, —CH 2 C(R 10 )(R 11 )—*, —CH 2 C(R 10 )(R 11 )—O—*, —CH 2 —O—C(R 10 )(R 11 )—* and —C(R 10 )(R 11 )—O—CH 2 —*, wherein the bond indicated by an asterisk is attached to the pyrazole ring; Z is as defined in the specification; R 10 is hydrogen and R 11 is (C 1 -C 3 )alkyl or —OH; or R 10 and R 11 are both (C 1 -C 3 )alkyl; or R 10 and R 11 taken together with the carbon atom to which they are attached form a (C 3 -C 5 )cycloalkyl ring.

  式(I)的化合物抑制CB1受体的正常信号活动，因此可用于治疗由CB1受体信号活动介导的疾病或症状，例如肥胖和超重的治疗，预防体重增加，直接或间接与肥胖和超重相关的疾病和症状的治疗：其中A1是氢，-COOH或四唑基；p和q独立地为0或1；A3是苯基或环烷基，其中任一可选地用R4和/或R5取代；R4和R5独立地为-R9，-CN，-F，-Cl，-Br，-OR9，-NR7R8，-NR7COR6，-NR7SO2R6，-COR6，-SR9，-SOR9或-SO2R6；R6是C1-C4烷基，环烷基，-CF3或-NR7R8；R7和R8独立地为氢，C1-C4烷基或环烷基；R9为氢，C1-C4烷基，C1-C4烷氧基，C1-C4烷氧基（C1-C4烷基）-，环烷基或完全或部分氟化的C1-C4烷基；R1(i)为键；（ii）为式-（CH2）aB1（ ）b的二价基团，其中a和b独立地为O，1，2或3，前提是a+b为1，2或3，B1为-CO-，-O-，-S-，-SO-，-SO2-，- -，-CHCH3-，-CHOH-或-NR7-；或（iii）为从-C（R10）（R11）- *，-C（R10）（R11）-O- *，-C（R10）（R11） - *，-C（R10）（R11） - O- *，- C（R10）（R11）- *，- C（R10）（R11）-O- *，- -O-C（R10）（R11）- *和-C（R10）（R11）-O- - *中选择的二价基团，其中由星号表示的键连接到吡唑环；Z如规范中所定义；R10为氢，R11为（C1-C3）烷基或-OH；或R10和R11均为（C1-C3）烷基；或R10和R11与它们连接的碳原子一起形成（C3-C5）环烷基环。
• Novel process for preparing picenadol
  申请人：ELI LILLY AND COMPANY

  公开号：EP0247639A2

  公开（公告）日：1987-12-02

  The present invention relates to processes for preparing precursors of picenadol, (±)3-(1,3α-dimethyl-4α-­propyl-4β-piperidinyl)phenol, hydrochloride, a known analgesic.

  本发明涉及一种已知镇痛剂--(±)3-(1,3α-二甲基-4α-丙基-4β-哌啶基)苯酚盐酸盐的前体的制备工艺。
• US7576076B2
  申请人：——

  公开号：US7576076B2

  公开（公告）日：2009-08-18