2-amino-3-cyclohexylthiophene | 120003-85-2

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 噻吩类
• 英文名称: 2-amino-3-cyclohexylthiophene
• 英文别名: 4-Cyclohexyl-2-thiophenamine；4-cyclohexylthiophen-2-amine
• CAS: 120003-85-2
• 化学式: C₁₀H₁₅NS
• 分子量: 181.302
• InChiKey: UJFVIKZVXQVMQZ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.8
• 重原子数：
  12
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.6
• 拓扑面积：
  54.3
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  苯那地平杂质9 、 2-amino-3-cyclohexylthiophene 、 叔丁醇 以13%的产率得到
  参考文献：
  名称：

  ADACHI, IKUO;YAMAMORI, TERUO;HIRAMATSU, YOSHIHARU;SAKAI, KATSUNORI;MIHARA+, CHEM. AND PHARM. BULL., 36,(1988) N1, C. 4389-4402

  摘要：

  DOI：

文献信息

• Studies on dihydropyridines. III. Synthesis of 4,7-dihydrothieno(2,3-b)pyridines with vasodilator and antihypertensive activities.
  作者：IKUO ADACHI、TERUO YAMAMORI、YOSHIHARU HIRAMATSU、KATSUNORI SAKAI、SHIN-ICHI MIHARA、MASARU KAWAKAMI、MASAO MASUI、OSAMU UNO、MOTOHIKO UEDA

  DOI：10.1248/cpb.36.4389

  日期：——

  A series of 4-aryl-4, 7-dihydrothieno [2, 3-b] pyridine-5-carboxylate derivatives (I) was synthesized and tested for binding affinity to Ca2+ channels in rat cerebral cortex membranes, coronary vasodilator effect in isolated guinea pig hearts, and antihypertensive activity in spontaneously hypertensive rats.Several compounds had potent coronary vasodilator and antihypertensive activities.The structure-ctivity relationships of the series indicated that a lipophilic 3-alkyl substituent with moderate bulkiness was effective for enhancing the pharmacological potencies.Among them, methyl 4, 7-dihydro-3-isobuty1-6-methy1-4-(3-nitrophenyl) thieno [2, 3-b] pyridine-5-carboxylate (S-312) was selected as a promising cardiovascular agent.The relationship between the absolute configuration of S-312 and its biological activities is also presented.

  合成了一系列4-芳基-4, 7-二氢噻吩[2, 3-b]吡啶-5-羧酸酯衍生物(I)，并测试了它们对大鼠大脑皮层膜中Ca2+通道的结合亲和力、在离体豚鼠心脏中的冠状动脉扩张作用以及在自发性高血压大鼠中的抗高血压活性。若干化合物具有强大的冠状动脉扩张和抗高血压活性。该系列的结构-活性关系表明，具有适中体积的脂溶性3-烷基取代基对增强药理效能是有效的。其中，甲基4, 7-二氢-3-异丁基-6-甲基-4-(3-硝基苯基)噻吩[2, 3-b]吡啶-5-羧酸酯(S-312)被选为一个有前景的心血管药物。还介绍了S-312的绝对构型与其生物活性之间的关系。
• ADACHI, IKUO;YAMAMORI, TERUO;HIRAMATSU, YOSHIHARU;SAKAI, KATSUNORI;MIHARA+, CHEM. AND PHARM. BULL., 36,(1988) N1, C. 4389-4402
  作者：ADACHI, IKUO、YAMAMORI, TERUO、HIRAMATSU, YOSHIHARU、SAKAI, KATSUNORI、MIHARA+

  DOI：——

  日期：——
• POLYMER, PROCESS AND USE
  申请人：DSM IP Assets B.V.

  公开号：EP2723799A1

  公开（公告）日：2014-04-30
• [EN] POLYMER, PROCESS AND USE<br/>[FR] POLYMÈRE ET PROCÉDÉ ET UTILISATION S'Y RAPPORTANT
  申请人：DSM IP ASSETS BV

  公开号：WO2012175622A1

  公开（公告）日：2012-12-27

  There is described a process for producing a gel free hyperbranched polyamide polymer P having a polydispersity of at least 1.1 and a weight average molecular weight of at least 300 daltons, having primary amino groups (useful as a crosslinker). The process comprises the step of reacting Reagent A, a compound comprising at least one amino group (-NH2) and one functional group selected from the group consisting of a further amino group (-NH2), thiol (-SH) and a secondary amine radical (-NHR); (where R denotes a hydrocarbo group) (=functional amine) and Reagent B, an alpha -beta unsaturated Michael-reactive ester comprising a plurality of ester groups (=diester);in a molar ratio of amine A to diester B greater than 1 but less than 3 (preferably 2.1 to 2.9);to form the polyamide in a two stage reaction Michael addition and then amidation. The amine in kept in excess with at least 5% of water by total weight of the amine and diester, a reaction temperature less than the boiling point of the amine; and is held under reduced pressure (30 mbar to 1 atms). Gelation does not occur even after substantially all ethylenic (-C=C- ) double bonds; and >95% ester [ -C(O)=O ] groups have reacted. This violates the Flory rules which predict a gel would form based on the number of functional groups present and their degree of conversion. These polymers may be used as a replacement for polyethylene imine (PEI) for example on plastics; in coatings, colours and/or adhesives; with metals; on textiles and fibres; in water treatment, paper, mineral processing and/or chemically modified Various chemical modifications and further reactions of these polymers are also described. A diverse range of other uses are also described including as additives for composite compositions, such as specialty additives for superplasticizers in concrete admixtures.