N-benzhydrylazetidine-2-carboxaldehyde | 72351-69-0

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: N-benzhydrylazetidine-2-carboxaldehyde
• 英文别名: 1-benzhydrylazetidine-2-carbaldehyde；1-diphenylmethyl-2-formylazetidine
• CAS: 72351-69-0
• 化学式: C₁₇H₁₇NO
• 分子量: 251.328
• InChiKey: DQVVUDMJLNXXOC-UHFFFAOYSA-N

物化性质

• 熔点：
  88-89 °C(Solv: hexane (110-54-3))
• 沸点：
  356.0±42.0 °C(Predicted)
• 密度：
  1.192±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  3.1
• 重原子数：
  19
• 可旋转键数：
  4
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.24
• 拓扑面积：
  20.3
• 氢给体数：
  0
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  N-benzhydrylazetidine-2-carboxaldehyde 在 Zn(N3)2-2 pyr 、 偶氮二甲酸二异丙酯 、 三苯基膦 作用下， 以 四氢呋喃 、 甲苯 为溶剂， 生成
  参考文献：
  名称：

  Synthesis and structure–activity relationships of aminoalkylazetidines as ORL1 receptor ligands

  摘要：

  A series of aminoalkylazetidines has been discovered as novel ORL1 receptor ligands. Structure-activity relationships have been investigated at the azetidine N and the alkyl side chain sites. Several potent and selective analogues have been identified. (C) 2002 Elsevier Science Ltd. All rights reserved.

  DOI：

  10.1016/s0960-894x(02)00652-2
• 作为产物：
  描述：

  1-二苯甲基-氮杂环丁烷-2-甲酸乙酯 在 二异丁基氢化铝 作用下， 以50%的产率得到N-benzhydrylazetidine-2-carboxaldehyde
  参考文献：
  名称：

  Synthesis and structure–activity relationships of aminoalkylazetidines as ORL1 receptor ligands

  摘要：

  A series of aminoalkylazetidines has been discovered as novel ORL1 receptor ligands. Structure-activity relationships have been investigated at the azetidine N and the alkyl side chain sites. Several potent and selective analogues have been identified. (C) 2002 Elsevier Science Ltd. All rights reserved.

  DOI：

  10.1016/s0960-894x(02)00652-2

文献信息

• Novel aminoglycoside derivatives
  申请人：Shionogi & Co., Ltd.

  公开号：US04200628A1

  公开（公告）日：1980-04-29

  Novel aminoglycoside derivatives and their salts containing 2-deoxystreptamine moiety, of which the 1-amino group is acylated by a group represented by the formula: ##STR1## (wherein R is 4 to 6 membered heterocyclic group containing 1 to 2 nitrogen atoms which may optionally be substituted.) effective in treatment of infectious diseases caused by gram positive and gram negative bacteria.

  含有2-脱氧链霉素结构单元的新型氨基糖苷衍生物及其盐，其中1-氨基团被表示为以下式的基团酰化：##STR1##（其中R是含有1到2个氮原子的4到6元杂环基团，可选择性地被取代）。对治疗由革兰氏阳性和革兰氏阴性细菌引起的传染病有效。
• Suppressing obesity and over-secretion of insulin with
  申请人：Takeda Chemical Industries, Ltd.

  公开号：US04349547A1

  公开（公告）日：1982-09-14

  2-(.alpha.-hydroxy-m-trifluoromethylbenzyl)azetidine and its physiologically acceptable acid addition salts have antiobesity action as well as suppressive action against oversecretion of insulin.

  2-（α-羟基-m-三氟甲基苯基）氮杂环丙烷及其生理上可接受的酸盐具有抗肥胖作用，同时还具有抑制胰岛素过度分泌的作用。
• Aminoglycoside derivatives, process for their manufacture, pharmaceutical compositions and carboxylic acids
  申请人：SHIONOGI & CO., LTD.

  公开号：EP0001643A2

  公开（公告）日：1979-05-02

  Aminoglycoside derivatives of the general formula (I) wherein R is an optionally substituted 4- to 6-membered heterocyclic group containing 1 or 2 nitrogen atoms; R is aminomethyl, hydroxymethyl, 1-aminoethyl, or 1-methylaminoethyl; R', R and R" are each hydrogen or hydroxy; π2 R3 and R° are each hydrogen or hydroxy; R4 is hydroxy or amino; R5 is amino or methylamino; R' is hydroxy or methyl; R" is hydrogen, hydroxymethyl, or carbamoyloxymetnyl; and the dotted line represents the optional presence of a double bond and their salts with acids, a process for their manufacture, pharmaceutical compositions having antibiotic activity and containing compounds of the general formula (I); furthermore carboxylic acids of the general formula (III) wherein R has the above meaning, useful as intermediates for preparing the compounds of the general formula (I).

  通式(I)的氨基糖苷衍生物 其中 R 是任选取代的含有 1 或 2 个氮原子的 4 至 6 元杂环基团； R 是氨甲基、羟甲基、1-氨基乙基或 1-甲基氨基乙基； R'、R 和 R" 均为氢或羟基； π2 R3 和 R° 均为氢或羟基； R4 是羟基或氨基 R5 是氨基或甲氨基 R' 是羟基或甲基； R" 是氢、羟甲基或氨基甲酰氧甲基；以及 虚线表示可选择存在的双键 及其与酸的盐类、其制造方法、具有抗生素活性并含有通式（I）化合物的药物组合物；以及通式（III）的羧酸 其中 R 具有上述含义，可用作制备通式（I）化合物的中间体。
• Azetidine derivative, its production, the derivative for use as an anti-obesity agent
  申请人：Takeda Chemical Industries, Ltd.

  公开号：EP0025880A1

  公开（公告）日：1981-04-01

  2-(α-Hydroxy-m-trifluoromethylbenzyl)azetidine and its physiologically acceptable acid addition salts have antiobesity action as well as suppressive action on over-secretion of insulin.

  2-(α-羟基-间三氟甲基苄基)氮杂环丁烷及其生理上可接受的酸加成盐具有抗肥胖和抑制胰岛素过度分泌的作用。
• MEGURO, KANJI;TAWADA, HIROYUKI;KAWAMATSU, YUTAKA;MATSUO, TAKAO, J. TAKEDA RES. LAB., 1981, 40, N 1-2, 1-11
  作者：MEGURO, KANJI、TAWADA, HIROYUKI、KAWAMATSU, YUTAKA、MATSUO, TAKAO

  DOI：——

  日期：——