trans-diazenedicarboxylic acid dipropyl ester | 2787-39-5

• 分子结构分类: 有机化合物 - 有机氮化合物
• 英文名称: trans-diazenedicarboxylic acid dipropyl ester
• 英文别名: trans-Azodikohlensaeure-dipropylester；trans-Diazendicarbonsaeure-dipropylester；propyl (NE)-N-propoxycarbonyliminocarbamate
• CAS: 2787-39-5
• 化学式: C₈H₁₄N₂O₄
• 分子量: 202.21
• InChiKey: JZXLRQAPALNNJI-MDZDMXLPSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.7
• 重原子数：
  14
• 可旋转键数：
  6
• 环数：
  0.0
• sp3杂化的碳原子比例：
  0.75
• 拓扑面积：
  77.3
• 氢给体数：
  0
• 氢受体数：
  4

反应信息

• 作为产物：
  描述：

  Hydrazin-dicarbonsaeure-di-n-propylester 在 水 、 氯 、 苯 作用下， 生成 trans-diazenedicarboxylic acid dipropyl ester
  参考文献：
  名称：

  Adsorption aus wässrigen Lösungen: Vergleich theoretischer Ansätze zur Vorhersage der Henry-Koeffizienten

  摘要：

  DOI：

  10.1002/1522-2640(200008)72:8<822::aid-cite822>3.0.co;2-3

文献信息

• METHOD FOR PREPARING AFATINIB AND INTERMEDIATE THEREOF
  申请人：Xu Xuenong

  公开号：US20160083373A1

  公开（公告）日：2016-03-24

  Revealed in the present invention is a method for preparing Afatinib (I): using 2-nitrile-4-[4-(N,N-dimethylamino)-I-oxo-2-buten-I-yl]amino-5-[(S)-(tetrahydrofuran-3-yl)oxy]aniline (II) and 4-fluoro-3-chloroaniline (III) as starting materials, and respectively performing a condensation and cyclization reaction with N,N-dimethylformamide dimethyl acetal (IV) to prepare Afatinib (I), wherein the method significantly reduces the manufacturing steps of Afatinib and greatly lower the costs. In addition, also provided in the present invention is a method for preparing an intermediate of Afatinib, wherein the method has a stable process, uses readily available starting materials, has a low cost, and all the reactions are classic reactions, suitable for meeting amplification requirements in the industry.

  本发明揭示了一种制备阿法替尼（I）的方法：使用2-腈基-4-[4-(N,N-二甲基氨基)-1-氧代-2-丁烯-1-基]氨基-5-[(S)-(四氢呋喃-3-基)氧基]苯胺（II）和4-氟-3-氯苯胺（III）作为起始原料，分别与N,N-二甲基甲酰胺二甲基缩醛（IV）进行缩合和环化反应制备阿法替尼（I），该方法显著减少了阿法替尼的制造步骤，大大降低了成本。此外，本发明还提供了一种制备阿法替尼中间体的方法，该方法具有稳定的工艺过程，使用易得的起始原料，成本低廉，并且所有反应均为经典反应，适合满足行业中的扩产需求。
• [EN] 3-PHENYL-4-HEXYNOIC ACID DERIVATIVES AS GPR40 AGONISTS<br/>[FR] DÉRIVÉS D'ACIDES 3-PHÉNYL-4-HEXINOÏQUES EN TANT QU'AGONISTES DE GPR40
  申请人：CELON PHARMA SA

  公开号：WO2019134984A1

  公开（公告）日：2019-07-11

  A compound of the formula (I)wherein R represents a straight or branched, primary or secondary acyclic hydrocarbyl C3–C15 group, which can be saturated or unsaturated, or a straight or branched, primary or secondary acyclic hydrocarbyl C3–C15 group, which can be saturated or unsaturated and wherein one or more of hydrogen atoms is replaced with fluorine atom; X represents hydrogen atom or halogen atom,and* denotes chiral center, and salts thereof. The compound is useful for the treatment of diseases mediated by GPR40, in particular type II diabetes. (I)

  式（I）的化合物，其中R代表直链或支链、一次或二次脂肪族C3-C15基团，可以是饱和或不饱和，或者直链或支链、一次或二次脂肪族C3-C15基团，可以是饱和或不饱和，其中一个或多个氢原子被氟原子取代；X代表氢原子或卤素原子，*表示手性中心，以及其盐。该化合物对于治疗由GPR40介导的疾病，特别是II型糖尿病，具有用处。
• NOVEL PROCESS FOR PREPARING PHENYLCYCLOPROPYLAMINE DERIVATIVES USING NOVEL INTERMEDIATES
  申请人：Khile Anil Shahaji

  公开号：US20130150577A1

  公开（公告）日：2013-06-13

  Provided herein is a novel process for the preparation of phenylcyclopropylamine derivatives, which are useful intermediates in the preparation of triazolo[4,5-d]pyrimidine compounds. Provided particularly herein is a novel, commercially viable and industrially advantageous process for the preparation of a substantially pure ticagrelor intermediate, trans-(1R,2S)-2-(3,4-difluorophenyl)-cyclopropylamine. The intermediate is useful for preparing ticagrelor, or a pharmaceutically acceptable salt thereof, in high yield and purity.

  本文提供了一种新颖的制备苯基环丙胺衍生物的过程，这些衍生物在三唑并[4,5-d]嘧啶化合物的制备中是有用的中间体。特别提供了一种新颖的、商业可行且在工业上具有优势的过程，用于制备一种基本纯净的替卡格雷中间体，即trans-(1R,2S)-2-(3,4-二氟苯基)-环丙胺。该中间体可用于高产率和纯度地制备替卡格雷或其药学上可接受的盐。
• Process for selectively synthesising 3 alpha-hydroxychlormadinone acetate
  申请人：Otten Thomas

  公开号：US20090318720A1

  公开（公告）日：2009-12-24

  The invention relates to a process for synthesising 3α-hydroxychlormadinone acetate.

  该发明涉及一种合成3α-羟基氯马酮醋酸酯的过程。
• Benzylamine analogues
  申请人：SANKYO COMPANY, LIMITED

  公开号：US20040067981A1

  公开（公告）日：2004-04-08

  A compound of the formula (I): 1 wherein R 1 represents C 1 -C 6 alkyl, amino (C 1 -C 6 alkyl)amino, di(C 1 -C 6 alkyl) amino or a nitrogen-containing saturated heterocyclic; R 2 and R 3 are the same or different and represent hydrogen or C 1 -C 6 alkyl; R a represents C 1 -C 6 alkyl or C 2 -C 6 alkenyl or together with R 2 represents a C 1 -C 3 alkylene; Arom represents aryl or heteroaryl; A represents a C 1 -C 6 alkylene; E represents a single bond, oxygen, sulfur or R 4 NR 4 —, wherein R 4 is hydrogen or C 1 -C 7 alkenoyl; X 1 and X 2 are the same or different and represent oxygen or sulfur; or a pharmacologically acceptable salt or ester thereof. The compound has superior acetylcholinesterase inhibitory action and selective serotonin reuptake inhibitory action, and is useful for treating or preventing Alzheimer's disease, depression, Huntington's chorea, Pick's disease, tardive dyskinesia, compulsive disorders or panic disorders.

  化合物的化学式为（I）：1，其中R1代表C1-C6烷基，氨基（C1-C6烷基）氨基，二（C1-C6烷基）氨基或含氮饱和杂环；R2和R3相同或不同，代表氢或C1-C6烷基；R代表C1-C6烷基或C2-C6烯基或与R2一起代表C1-C3烷基；Arom代表芳基或杂芳基；A代表C1-C6烷基；E代表单键，氧，硫或R4NR4—，其中R4为氢或C1-C7烯酰基；X1和X2相同或不同，代表氧或硫；或其药学上可接受的盐或酯。该化合物具有优异的乙酰胆碱酯酶抑制作用和选择性5-羟色胺再摄取抑制作用，并可用于治疗或预防阿尔茨海默病、抑郁症、亨廷顿舞蹈症、皮克病、迟发性运动障碍、强迫性障碍或惊恐障碍。