(S)-1-Ethyl-2-methylpropylamin | 178962-87-3

• 分子结构分类: 有机化合物 - 有机氮化合物
• 英文名称: (S)-1-Ethyl-2-methylpropylamin
• 英文别名: (3S)-2-methylpentan-3-amine
• CAS: 178962-87-3
• 化学式: C₆H₁₅N
• 分子量: 101.192
• InChiKey: JYNQKCFJPQEXSL-LURJTMIESA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.6
• 重原子数：
  7
• 可旋转键数：
  2
• 环数：
  0.0
• sp3杂化的碳原子比例：
  1.0
• 拓扑面积：
  26
• 氢给体数：
  1
• 氢受体数：
  1

反应信息

• 作为反应物：
  描述：

  (S)-1-Ethyl-2-methylpropylamin 在 盐酸 作用下， 以 乙醇 、 水 为溶剂， 反应 3.0h， 生成 (R)-2-methylpentan-3-amine hydrochloride
  参考文献：
  名称：

  碘化铵和氢催化钌催化简单脂肪族酮的不对称直接还原胺化

  摘要：

  在脂肪族酮与伯胺的直接不对称还原胺化上：通过使用Ru-Binaphane作为催化剂和NH 4 I作为胺源，可以胺化中等ee值高达74％的前手性脂肪族酮。

  DOI：

  10.1002/ejoc.202000750
• 作为产物：
  描述：

  2-甲基-3-戊酮 在 碘化铵 、 [RuHCl(CO)(PPh₃)₃] 、 (S,S)-f-binaphane 、 氢气 作用下， 以 甲醇 、 甲苯 为溶剂， 80.0 ℃ 、3.0 MPa 条件下， 反应 36.0h， 以62%的产率得到
  参考文献：
  名称：

  碘化铵和氢催化钌催化简单脂肪族酮的不对称直接还原胺化

  摘要：

  在脂肪族酮与伯胺的直接不对称还原胺化上：通过使用Ru-Binaphane作为催化剂和NH 4 I作为胺源，可以胺化中等ee值高达74％的前手性脂肪族酮。

  DOI：

  10.1002/ejoc.202000750

文献信息

• Carboxamide Derivatives and Use Thereof
  申请人：PURDUE PHARMA L.P.

  公开号：US20160031873A1

  公开（公告）日：2016-02-04

  The present disclosure provides substituted pyridyl-, pyrimidinyl-, pyrazinyl-, pyridazinyl-, and triazinyl-based carboxamides of Formula I-A: R 10 Z-HET-E I-A and the pharmaceutically acceptable salts and solvates thereof, wherein Z, HET, R 10 and E are defined as set forth in the specification. The present disclosure is also directed to the use of compounds of Formula I-A to treat a disorder responsive to the blockade of sodium channels. Compounds of the present disclosure are especially useful for treating pain.

  本公开提供了公式I-A的取代吡啶基、嘧啶基、吡嗪基、吡啉基和三嗪基羧酰胺，以及其药学上可接受的盐和溶剂化合物，其中Z、HET、R10和E如规范中所定义。本公开还涉及使用公式I-A的化合物治疗对钠通道阻滞有响应的疾病。本公开的化合物特别适用于治疗疼痛。
• PROTEIN-POLYMER-DRUG CONJUGATES
  申请人：MERSANA THERAPEUTICS, INC.

  公开号：US20150044160A1

  公开（公告）日：2015-02-12

  A drug conjugate is provided herein. The conjugate comprises a protein based recognition-molecule (PBRM) and a polymeric carrier substituted with one or more -L D -D, the protein based recognition-molecule being connected to the polymeric carrier by L P . Each occurrence of D is independently a therapeutic agent having a molecular weight ≦5 kDa. L D and L P are linkers connecting the therapeutic agent and PBRM to the polymeric carrier respectively. Also disclosed are polymeric scaffolds useful for conjugating with a PBRM to form a polymer-drug-PBRM conjugate described herein, compositions comprising the conjugates, methods of their preparation, and methods of treating various disorders with the conjugates or their compositions.

  本文提供一种药物偶联物。该偶联物包括一种基于蛋白质的识别分子（PBRM）和一种聚合物载体，其取代了一个或多个-LD-D，其中，基于蛋白质的识别分子通过LP连接到聚合物载体上。每个D的出现都是独立的，其分子量≦5 kDa，是一种治疗剂。LD和LP是连接治疗剂和PBRM到聚合物载体的连接体。还公开了用于与PBRM偶联形成聚合物-药物-PBRM偶联物的聚合物支架，包括所述偶联物的组合物，其制备方法以及使用偶联物或其组合物治疗各种疾病的方法。
• NOVEL NICOTINAMIDE DERIVATIVE OR SALT THEREOF
  申请人：FUJIWARA Hideyasu

  公开号：US20130116430A1

  公开（公告）日：2013-05-09

  An object of the present invention is to provide to a compound and a pharmaceutical composition, which have excellent Syk-inhibitory activity. The present invention provides a nicotinamide derivative represented by the following formula (I) (wherein R 1 represents a halogen atom; R 2 represents a C 1-12 alkyl group, a C 2-12 alkenyl group, a C 2-12 alkynyl group, a C 3-8 cycloalkyl group, an aryl group, an ar-C 1-6 alkyl group or a heterocyclic group, each optionally having at least one substituent; R 3 represents an aryl group or a heterocyclic group each optionally having at least one substituent; and R 4 and R 5 each independently represent a hydrogen atom; and R 2 and R 4 may form a cyclic amino group optionally having at least one substituent together with the nitrogen atom to which they bind) or a salt thereof, and a pharmaceutical composition for use in the treatment of a Syk-related disease which comprises the nicotinamide derivative or a salt thereof.

  本发明的目的是提供一种具有优异的Syk抑制活性的化合物和制药组合物。本发明提供了一种由以下式(I)表示的烟酰胺衍生物（其中R1表示卤素原子；R2表示C1-12烷基、C2-12烯基、C2-12炔基、C3-8环烷基、芳基、芳基-C1-6烷基或杂环基，每种均可选地具有至少一个取代基；R3表示芳基或杂环基，每种均可选地具有至少一个取代基；R4和R5各自独立地表示氢原子；且R2和R4可以与它们结合的氮原子一起形成具有至少一个取代基的环状氨基团）或其盐，并且用于治疗Syk相关疾病的制药组合物包括该烟酰胺衍生物或其盐。
• THERAPEUTIC COMPOUNDS
  申请人：GILEAD SCIENCES, INC.

  公开号：US20140221421A1

  公开（公告）日：2014-08-07

  Compounds of formula I: or salts thereof are disclosed. Also disclosed are pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula I, intermediates useful for preparing compounds of formula I and therapeutic methods for treating a Retroviridae viral infection including an infection caused by the HIV virus.

  本发明揭示了公式I的化合物或其盐。还揭示了包含公式I化合物的制药组合物，制备公式I化合物的方法，用于制备公式I化合物的中间体以及治疗Retroviridae病毒感染的治疗方法，包括由HIV病毒引起的感染。
• NOVEL MORPHOLINE DERIVATIVE OR SALT THEREOF
  申请人：Fujifilm Corporation

  公开号：EP3042900A1

  公开（公告）日：2016-07-13

  There is provided a morpholine derivative represented by General Formula [1A] or a salt thereof. (In the formula, a ring A represents a ring represented by General Formula [I]; * represents a bonding position; Z2 represents CH or the like; Z1 represents CR6 or the like; R6 represents a hydrogen atom or the like; X1 represents CHR7 or the like; R7 represents a hydrogen atom or the like; X2 represents CH2 or the like; R1 and R2 are the same as or different from each other, and each of R1 and R2 represents a hydrogen atom or the like; R3, R4 and R5 are the same as or different from each other, and each of R3, R4, and R5 represents a hydrogen atom, NRaRb, or the like; and each of Ra and Rb represents a hydrogen atom, a C1-8 alkyl group which may have a substituent, or the like.)

  提供了通式[1A]代表的吗啉衍生物或其盐。 (式中，环 A 代表通式[I]所代表的环；* 代表键合位置；Z2 代表 CH 或类似物；Z1 代表 CR6 或类似物；R6 代表氢原子或类似物；X1 代表 CHR7 或类似物；R7 代表氢原子或类似物；X2 代表 CH2 或类似物；R1和R2彼此相同或不同，且R1和R2各自代表氢原子或类似物；R3、R4和R5彼此相同或不同，且R3、R4和R5各自代表氢原子、NRaRb或类似物；Ra和Rb各自代表氢原子、可能具有取代基的C1-8烷基或类似物。)