N-methyl-alpha-(3-methyl-2-thienyl)benzeneethanamine | 143380-26-1

• 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-methyl-alpha-(3-methyl-2-thienyl)benzeneethanamine
• 英文别名: N-methyl-1-(3-methylthiophen-2-yl)-2-phenylethanamine
• CAS: 143380-26-1
• 化学式: C₁₄H₁₇NS
• 分子量: 231.36
• InChiKey: HGMNEJVNLRBEIU-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.4
• 重原子数：
  16
• 可旋转键数：
  4
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.29
• 拓扑面积：
  40.3
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  N-methyl-alpha-(3-methyl-2-thienyl)benzeneethanamine 、 N-ethyl-alpha-(2-thienyl)benzeneethanamine 以or N-ethyl-α-(3-methyl-2-thienyl)benzeneethanamine for the α-(3-methyl-2-thienyl)benzeneethanamine results in the preparation of的产率得到N-ethyl-alpha-(3-methyl-2-thienyl)benzeneethanamine
  参考文献：
  名称：

  (2-thienyl)alkylamine derivatives having neuroprotective properties

  摘要：

  公式I的化合物，##STR1## 其中：R.sub.1代表氢或C.sub.1-6烷基，R.sub.2代表氢，C.sub.1-6烷基，C.sub.3-6烯基，C.sub.3-6炔基或C.sub.3-6环烷基，R.sub.3代表氢，羟基，C.sub.1-6烷基，C.sub.1-6烷氧基，卤素，三氟甲基，氨基，低烷基氨基或二低烷基氨基中选择的一种或多种基团，R.sub.4代表氢或C.sub.1-6烷基中选择的一种或多种基团，A代表α-氨基酸酰基或烷氧羰基基团，及其药学上可接受的盐作为药物具有用途，特别是它们具有N-甲基-(d)-天门冬氨酸（NMDA）阻滞作用，并可用于治疗和/或预防神经系统疾病，如中风，脑缺血，脑瘫，低血糖，癫痫，阿尔茨海默病，亨廷顿舞蹈症，奥利沃-腹侧-小脑萎缩，围产期窒息和缺氧等。

  公开号：

  US05109017A1

文献信息

• (2-THIENYL) ALKYLAMINE DERIVATIVES HAVING NEUROPROTECTIVE PROPERTIES
  申请人：FISONS CORPORATION

  公开号：EP0557305A1

  公开（公告）日：1993-09-01
• US5109017A
  申请人：——

  公开号：US5109017A

  公开（公告）日：1992-04-28
• [EN] (2-THIENYL) ALKYLAMINE DERIVATIVES HAVING NEUROPROTECTIVE PROPERTIES
  申请人：FISONS CORPORATION

  公开号：WO1992005169A1

  公开（公告）日：1992-04-02

  (EN) Compounds of formula (I), in which: R1 represents hydrogen or C1-6 alkyl, R2 represents hydrogen, C1-6 alkyl, C3-6 alkenyl, C3-6 alkynyl or C3-6 cycloalkyl, R3 represents one or more radicals selected from hydrogen, hydroxy, C1-6 alkyl, C1-6 alkoxy, halogen, trifluoromethyl, amino, C1-6 alkylamino or di(C1-6 alkyl)amino, R4 represents one or more radicals selected from hydrogen or C1-6 alkyl, A represents hydrogen, C1-6 alkyl, COC(R5R6)N(R7R8) or COOC1-6 alkyl, R5 represents hydrogen, C1-6 alkyl, hydroxy-C1-2 alkyl, mercaptomethyl, (methylthio)C1-2 alkyl, carboxy-C1-2 alkyl, 2-(C1-3 alkoxy)ethyl, (aminocarbonyl)C1-2 alkyl, amino-C1-4 alkyl, 3-imidazolylmethyl, phenylmethyl or (4-hydroxyphenyl)-methyl, or in addition, R5 together with the adjacent nitrogen may represent a piperidine, pyrrolidine or a 2-pyrrolidinone ring, R6, R7 and R8 independently represent hydrogen or C1-6 alkyl, or in addition, R7 and R8 taken together with the nitrogen to which they are attached may represent a C4-5 N heterocyclic ring, and pharmaceutically acceptable acid addition salts thereof, are useful as pharmaceuticals; in particular they possess N-methyl-(D)-aspartate blocking properties and are useful in the treatment and/or prevention of neurological disorders.(FR) Composés de la formule (I) dans laquelle: R1 représente hydrogène ou C1-6 alkyle, R2 représente hydrogène, C1-6 alkyle, C3-6 alcényle, C3-6 alcényle ou C3-6 cycloalkyle, R3 représente un ou plusieurs radicaux choisis parmi hydrogène, hydroxy, C1-6 alkyle, C1-6 alcoxy, halogène, trifluorométhyle, amino, C1-6 alkylamino ou di (C1-6 alkyle) amino, R4 représente un ou plusieurs radicaux choisis parmi hydrogène ou C1-6 alkyle, A représente hydrogène, C1-6 alkyle, COC (R5R6)N (R7R8) ou COOC1-6 alkyle, R5 représente hydrogène, C1-6 alkyle, hydroxy-C1-2 alkyle, mercaptométhyle, (méthylthio)C1-2 alkyle, carboxy-C1-2 alkyle, 2-(C1-3alcoxy)éthyle, (aminocarbonyle)C1-2 alkyle, amino-C1-4 alkyle, 3-imidazolylméthyle, phénylméthyle ou (4-hydroxyphényle)-méthyle, ou en outre, R5 avec l'azote adjacent peut représenter un anneau de pipéridine, de pyrrolidine ou de 2-pyrrolidinone, R6, R7 et R8 représentent indépendamment hydrogène ou C1-6 alkyle, ou en outre, R7 et R8, pris avec l'azote auquel ils sont attachés, peuvent représenter un anneau C4-5 hétérocyclique, et des sels d'addition acides pharmaceutiquement acceptables desdites substances. Les composés de la formule (1) sont des produits pharmaceutiques utiles; ils possèdent notamment des propriétés de blocage de N-méthyle-(D)-aspartate et sont utiles dans le traitement et/ou la prévention de troubles neurologiques.
• (2-thienyl)alkylamine derivatives having neuroprotective properties
  申请人：Fisons Corporation

  公开号：US05109017A1

  公开（公告）日：1992-04-28

  Compounds of the formula I, ##STR1## in which: R.sub.1 represents hydrogen or C.sub.1-6 alkyl, R.sub.2 represents hydrogen, C.sub.1-6 alkyl, C.sub.3-6 alkenyl, C.sub.3-6 alkynyl or C.sub.3-6 cycloalkyl, R.sub.3 represents one or more radicals selected from hydrogen, hydroxy, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, halogen, trifluoromethyl, amino, lower alkylamino or dilower alkylamino, R.sub.4 represents one or more radicals selected from hydrogen or C.sub.1-6 alkyl, A represents an alpha-amino acid acyl group or an alkoxycarbonyl group, and pharmaceutically acceptable salts thereof are useful as pharmaceuticals, in particular they possess N-methyl-(d)-aspartate (NMDA) blocking properties and are useful in the treatment and/or prevention of neurological disorders such as stroke, cerebral ischaemia, cerebral palsy, hypoglycaemia, epilepsy, Alzheimer's disease, Huntington's chorea, Olivo-ponto-cerebellar atrophy, perinatal asphyxia and anoxia.

  公式I的化合物，##STR1## 其中：R.sub.1代表氢或C.sub.1-6烷基，R.sub.2代表氢，C.sub.1-6烷基，C.sub.3-6烯基，C.sub.3-6炔基或C.sub.3-6环烷基，R.sub.3代表氢，羟基，C.sub.1-6烷基，C.sub.1-6烷氧基，卤素，三氟甲基，氨基，低烷基氨基或二低烷基氨基中选择的一种或多种基团，R.sub.4代表氢或C.sub.1-6烷基中选择的一种或多种基团，A代表α-氨基酸酰基或烷氧羰基基团，及其药学上可接受的盐作为药物具有用途，特别是它们具有N-甲基-(d)-天门冬氨酸（NMDA）阻滞作用，并可用于治疗和/或预防神经系统疾病，如中风，脑缺血，脑瘫，低血糖，癫痫，阿尔茨海默病，亨廷顿舞蹈症，奥利沃-腹侧-小脑萎缩，围产期窒息和缺氧等。