Piflutixol | 60756-96-9

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯并噻喃类
• 英文名称: Piflutixol
• 英文别名: 2-[1-[(3Z)-3-[6-fluoro-2-(trifluoromethyl)thioxanthen-9-ylidene]propyl]piperidin-4-yl]ethanol
• CAS: 60756-96-9
• 化学式: C₂₄H₂₅F₄NOS
• 分子量: 451.5
• InChiKey: CCUOZZURYIZOKX-UYKKPYKBSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  5.9
• 重原子数：
  31
• 可旋转键数：
  5
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.42
• 拓扑面积：
  48.8
• 氢给体数：
  1
• 氢受体数：
  7

文献信息

• Xanthone and thioxanthone derivatives, their preparation and pharmaceutical compositions containing them
  申请人：KEFALAS A/S

  公开号：EP0005607A1

  公开（公告）日：1979-11-28

  Xanthone- and thioxanthone derivatives of the formula: wherein X is a halogen atom, an alkyl group, an alkyloxy group, said alkyl and alkyloxy groups having from one to four carbon atoms inclusive, a methylthio group, a methyl- suphonyl group, a dimethylsulphamoyl group, a trifluoromethyl group, or an acetyl group; Y is hydrogen, fluorine or a methyl group; Z is oxygen or sulphur; n is an integer from zero to three inclusive, and R is a cycloalkyl group with from four to six carbon atoms inclusive in the ring, substituted with from one to four substituents selected from optionally esterified hydroxy- or hydroxymethyl groups, methyl groups, amono groups, acetamino groups, mesylamino groups or oxo groups, a five-or six-membered saturated heterocyclic ring having one or two hetero atoms selected from oxygen and nitrogen atoms and being optionally substituted with an optionally esterified hydroxy group, any esterified hydroxy group present being an ester of an aliphatic carboxylic acid having from ten to twentytwo carbon atoms inclusive, or an oxo group, as well as their non-toxic pharmaceutically acceptable acid addition salts. Methods for the preparation of compounds of Formula I and novel intermediates used in said methods. The novel compounds of Formula I having strong, and sometimes very long-lasting neuroleptic effects, at the same time showing relatively low extrapyrimidal side effects, a low acute toxicity and moderately strong anticholinergic effects and comparatively low undesired sedative effects.

  式中的氧雜蔥酮和硫雜蔥酮衍生物： 其中 X 是卤素原子、烷基、烷氧基（烷基和烷氧基的碳原子数从 1 个到 4 个不等）、甲硫基、甲上酰基、二甲基氨基磺酰基、三氟甲基或乙酰基； Y 是氢、氟或甲基 Z 是氧或硫； n 是 0 至 3（包括 3）的整数，且 R 是环烷基，在环中有 4 至 6 个碳原子，被 1 至 4 个取代基取代，这些取代基可选 自经酯化的羟基或羟甲基、甲基、氨基、乙酰氨基、间氨基或氧代基、五元或六元饱和杂环，具有一个或两个选自氧原子和氮原子的杂原子，并被任选的酯化羟基取代，其中任何酯化羟基均为具有 10 至 22 个碳原子（含）的脂肪族羧酸的酯或氧代基团，以及它们的无毒药学上可接受的酸加成盐。 式 I 化合物的制备方法以及用于上述方法的新型中间体。 式 I 的新型化合物具有较强的，有时是非常持久的神经安定作用，同时显示出相对较低的嘧啶外副作用、较低的急性毒性和中等强度的抗胆碱能作用，以及相对较低的不期望的镇静作用。
• US4275209A
  申请人：——

  公开号：US4275209A

  公开（公告）日：1981-06-23
• US4285956A
  申请人：——

  公开号：US4285956A

  公开（公告）日：1981-08-25
• US4309429A
  申请人：——

  公开号：US4309429A

  公开（公告）日：1982-01-05