trans-N-Boc-2-Methyl-6-Piperidinecarboxaldehyde | 1010076-44-4

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 哌啶类
• 英文名称: trans-N-Boc-2-Methyl-6-Piperidinecarboxaldehyde
• 英文别名: (2R,6S)-tert-butyl 2-formyl-6-methyl-1-piperidinecarboxylate；tert-butyl 2-formyl-6-methylpiperidine-1-carboxylate
• CAS: 1010076-44-4
• 化学式: C₁₂H₂₁NO₃
• 分子量: 227.304
• InChiKey: MEPVKWLQCNICCR-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2
• 重原子数：
  16
• 可旋转键数：
  3
• 环数：
  1.0
• 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

• 作为反应物：
  描述：

  trans-N-Boc-2-Methyl-6-Piperidinecarboxaldehyde 、 甲基三苯基溴化膦 在 正丁基锂 作用下， 以 四氢呋喃 、 乙酸乙酯 为溶剂， 以2.53 g (87%)的产率得到trans-N-Boc-2-(1-pentenyl)-6-methylpiperidine
  参考文献：
  名称：

  Solenopsin derivatives and analogues as fire ant suppressants

  摘要：

  本发明涉及溶蚁素生物碱衍生物，属于结构为trans-2,6-二取代哌啶的化合物：其中R1和R2选自C1至C20饱和或不饱和的直链、环状或支链取代或未取代的碳氢化合物基团或取代或未取代的芳香基团，或酯基。在某些首选实施方案中，如果R1或R2含有不饱和基团，如烯基基团，则烯基基团中的双键最好位于与哌啶环结合的碳原子和相邻碳原子（α和β碳）之间的碳氢链中。

  公开号：

  US06369078B1
• 作为产物：
  描述：

  (S)-(+)-N-(叔丁氧羰基)-2-甲基哌啶 在 四甲基乙二胺 、 ammonium chloride 作用下， 以 乙醚 、 N,N-二甲基甲酰胺 为溶剂， 以55%的产率得到trans-N-Boc-2-Methyl-6-Piperidinecarboxaldehyde
  参考文献：
  名称：

  Hydronaphtho[2,3-c]furan derivatives and process for the preparation thereof

  摘要：

  用于制备表现为肌胆碱M2受体拮抗作用的希巴辛的中间体，为通式（1）所代表的氢代萘并[2,3-c]呋喃衍生物或其制备的中间体：其中R1是较低的烷基或芳基；R2是氢、较低的烷基或芳基；R3和R4一起代表氧或亚甲基，或者R4是羟基、较低的烷氧基、芳基氧基或较低的酰氧基，R3是氢；R5和R6一起代表氧，或者R6是羟基、较低的烷氧基、芳基氧基或较低的酰氧基，R5是氢；其中任一虚线是单键，另一虚线是双键，或者两者都是单键。

  公开号：

  US06392059B1

文献信息

• Derivatives of N-[phenyl(alkylpiperidine-2-yl)methyl]benzamide, preparation method thereof and application of same in therapeutics
  申请人：Dargazanli Gihad

  公开号：US20060223861A1

  公开（公告）日：2006-10-05

  Compounds of formula (I) as defined herein: are useful for treating behavioral disorders associated with dementia, psychoses, in particular schizophrenia (deficient form and productive form) and acute or chronic extrapyramidal symptoms induced by neuroleptics; for the treatment of various forms of anxiety, panic attacks, phobias, and compulsive obsessive disorders; for treating various forms of depression, including psychotic depression; for treating disorders caused by alcohol abuse or weaning from alcohol, sexual behavior disorders, eating disorders and for treating migraine. Moreover, the compounds of the invention may be used for treating painful muscle contracture in rheumatology and in acute spinal pathology; for treating spastic contractures of medullary or cerebral origin; for the symptomatic treatment of acute and subacute pain of light to moderate intensity; for treating intense and/or chronic pain, neurogenic pain and intractable pain; for treating Parkinson's disease and Parkinson-like symptoms of neurodegenerative origin or induced by neuroleptics; for treating partial primary and secondary generalized epilepsy of simple or complex symptomology, mixed forms and other epileptic syndromes in addition to another antiepileptic treatment, or in monotherapy, for the treatment of sleep apnea, and for neuroprotection.

  本发明的化合物（I）的化学式如下：用于治疗与痴呆相关的行为障碍，精神病，特别是精神分裂症（缺乏型和产生型）以及由神经类药物引起的急性或慢性锥体外症状；用于治疗各种形式的焦虑、恐慌发作、恐惧症和强迫性妄想症；用于治疗各种形式的抑郁症，包括精神抑郁症；用于治疗由酒精滥用或戒酒引起的障碍，性行为障碍，进食障碍以及治疗偏头痛。此外，本发明的化合物可用于治疗风湿病学中的疼痛性肌肉挛缩和急性脊柱病理学；用于治疗由脊髓或大脑起源的痉挛性挛缩；用于对轻到中度强度的急性和亚急性疼痛进行症状性治疗；用于治疗剧烈和/或慢性疼痛，神经源性疼痛和难治性疼痛；用于治疗帕金森病和由神经类药物引起的神经退行性症状或帕金森样症状；用于治疗简单或复杂症状学、混合形式和其他癫痫综合征的部分原发性和继发性全身性癫痫，除了其他抗癫痫治疗外，还可单独使用，用于治疗睡眠呼吸暂停症，以及用于神经保护。
• Decahydronaphtho[2,3-c]furan derivatives
  申请人：Takadoi Masanori

  公开号：US20050124658A1

  公开（公告）日：2005-06-09

  The invention provides useful novel analogues of himbacine, being an alkaloid with potent and selective antagonism against muscarine M 2 receptor. Hydronaphtho [2,3-c] furan derivatives represented by a following general formula (1) and their acid addition salts.

  该发明提供了对甲胆碱M2受体具有强效和选择性拮抗作用的有用的新型希姆巴辛类似物。由下列一般式（1）代表的羟基萘并[2,3-c]呋喃衍生物及其酸盐。
• Solenopsin derivatives and analogues as fire ant suppressants
  申请人：——

  公开号：US06369078B1

  公开（公告）日：2002-04-09

  The present invention relates to solenopsin alkaloid derivatives which are trans-2,6-disubstituted piperidines according to the structure: wherein R1 and R2 are selected from a C1 to C20 saturated or unsaturated linear, cyclic or branch-chained substituted or unsubstituted hydrocarbon group or a substituted or unsubstituted aromatic group, or an ester group. In certain preferred embodiments, where R1 or R2 contains an unsaturated group, such as an alkenyl group, the double bond in the alkenyl group preferably is found in the hydrocarbon chain between the carbon atom bonded to the piperidine ring and the adjacent carbon atom (&agr; and &bgr; carbons).

  本发明涉及溶蚁素生物碱衍生物，属于结构为trans-2,6-二取代哌啶的化合物：其中R1和R2选自C1至C20饱和或不饱和的直链、环状或支链取代或未取代的碳氢化合物基团或取代或未取代的芳香基团，或酯基。在某些首选实施方案中，如果R1或R2含有不饱和基团，如烯基基团，则烯基基团中的双键最好位于与哌啶环结合的碳原子和相邻碳原子（α和β碳）之间的碳氢链中。
• Novel gamma secretase inhibitors
  申请人：Schering-Plough Corporation

  公开号：US20040171614A1

  公开（公告）日：2004-09-02

  This invention discloses novel gamma secretase inhibitors of the formula: 1 wherein: R 1 is a substituted aryl or substituted heteroaryl group; R 2 is an R 1 group, alkyl, —XC(O)Y, alkylene-XC(O)Y, cycloalkylene-X-C(O)—Y, —CH—X—C(O)—NR 3 —Y or —CH—X—C(O)—Y, wherein X and Y are as defined herein; each R 3 and each R 3A are independently H, or alkyl; R 11 is aryl, heteroaryl, alkyl, cycloalkyl, arylalkyl, arylcycloalkyl, heteroarylalkyl, heteroarylcycloalkyl, arylheterocycloalkyl, or alkoxyalkyl. Also disclosed is a method of treating Alzheimer's Disease using one or more compounds of the invention.

  这项发明揭示了一种新颖的伽玛分泌酶抑制剂，其化学式为：其中：R1为取代芳基或取代杂芳基；R2为R1基团、烷基、—XC(O)Y、烷基烯-XC(O)Y、环烷基烯-X-C(O)—Y、—CH—X—C(O)—NR3—Y或—CH—X—C(O)—Y，其中X和Y如本文中所定义；每个R3和每个R3A独立地为H或烷基；R11为芳基、杂芳基、烷基、环烷基、芳基烷基、芳基环烷基、杂芳基烷基、杂芳基环烷基、芳基杂环烷基或烷氧基烷基。还公开了使用该发明的一个或多个化合物治疗阿尔茨海默病的方法。
• [EN] GAMMA SECRETASE INHIBITORS<br/>[FR] INHIBITEURS DE LA GAMMA-SECRETASE
  申请人：SCHERING CORP

  公开号：WO2003066592A1

  公开（公告）日：2003-08-14

  This invention discloses novel gamma secretase inhibitors of the formula:(Chemical formula should be inserted here as it appears on abstract in paper form)wherein: R1 is a substituted aryl or substituted heteroaryl group; R2 is an R1 group, alkyl, -X(CO)Y, or alkylene-X(CO)Y wherein X and Y are as defined herein; each R3 and each R3A are independently H, or alkyl; R11 is aryl, heteroaryl, alkyl, cycloalkyl, arylalkyl, arylcycloalkyl, heteroarylalkyl, heteroarylcycloalkyl, arylheterocycloalkyl, or alkoxyalkyl. Also disclosed is a method of treating Alzheimer s Disease using one or more compounds of the invention.

  本发明公开了一种新型γ-分泌酶抑制剂，其化学式为：（化学式应按照论文形式插入此处） 其中：R1是取代芳基或取代杂环基；R2是R1基团，烷基，-X（CO）Y，或烷基-X（CO）Y，其中X和Y如定义所述；每个R3和每个R3A独立地是氢或烷基；R11是芳基，杂环基，烷基，环烷基，芳基烷基，芳基环烷基，杂环基烷基，杂环基环烷基，芳基杂环环烷基或烷氧基烷基。本发明还公开了使用本发明的一种或多种化合物治疗阿尔茨海默病的方法。