2-(3-吡啶)噻唑烷-4-羧酸 | 59777-95-6

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 中文名称: 2-(3-吡啶)噻唑烷-4-羧酸
• 中文别名: 2-(3-吡啶基)噻唑烷-4-羧酸
• 英文名称: (4-R)-2-(pyridin-3-yl)thiazolidine-4-carboxylic acid
• 英文别名: 2-(pyridin-3-yl)-thiazolidine-4-carboxylic acid；2-(3-pyridinyl)-4-thiazolidinecarboxylic acid；2-pyridin-3-yl-thiazolidine-4-carboxylic acid；2-(pyridin-3-yl)thiazolidine-4-carboxylic acid；2-(3-pyridyl)thiazolidine-4-carboxylic acid；2--thiazolidin-carbonsaeure-(4)；2-(Pyridinium-3-yl)-1,3-thiazolidine-4-carboxylate；2-pyridin-1-ium-3-yl-1,3-thiazolidine-4-carboxylate
• CAS: 59777-95-6
• 化学式: C₉H₁₀N₂O₂S
• mdl: MFCD01115161
• 分子量: 210.257
• InChiKey: FSNGLHIMQHWTNF-UHFFFAOYSA-N

物化性质

• 熔点：
  136-137 °C
• 沸点：
  468.2±45.0 °C(Predicted)
• 密度：
  1.366±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  -1.9
• 重原子数：
  14
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.333
• 拓扑面积：
  87.5
• 氢给体数：
  2
• 氢受体数：
  5

安全信息

• 危险等级：
  IRRITANT
• 危险品标志：
  Xi
• 海关编码：
  2934999090
• 储存条件：
  | 室温 |

反应信息

• 作为反应物：
  描述：

  2-(3-吡啶)噻唑烷-4-羧酸 在 苯胺 作用下， 生成 N-Phenyl-2-(pyridin-3-yl)thiazolidine-4-carboxamide dihydrochloride
  参考文献：
  名称：

  Saturated heterocyclic carboxamide derivatives

  摘要：

  以下是通用公式（I）的饱和杂环羧酰胺衍生物及其盐，具有血小板活化因子（PAF）拮抗活性。

  公开号：

  US04987132A1
• 作为产物：
  描述：

  3-吡啶甲醛 、 DL-半胱氨酸 生成 2-(3-吡啶)噻唑烷-4-羧酸
  参考文献：
  名称：

  Saturated heterocyclic carboxamide derivatives

  摘要：

  以下是通式（I）的饱和杂环羧酰胺衍生物及其盐，具有血小板活化因子（PAF）拮抗活性。 ##STR1##

  公开号：

  US04987132A1
• 作为试剂：
  描述：

  二碳酸二叔丁酯 在 sodium hydroxide 作用下， 以 1,4-二氧六环 、 2-(3-吡啶)噻唑烷-4-羧酸 为溶剂， 以80%的产率得到3-tert-butoxycarbonyl-2-(pyridin-3-yl)-4-thiazolidinecarboxylic acid
  参考文献：
  名称：

  Platelet activating antagonists

  摘要：

  在1-或3位被(pyrid-3 yl)thiazolid-4-yl)alkyl-, (pyrid-3-yl)thiazolid-4-oyl)-, (pyrid-3-yl)dithiolan-4-yl)alkyl-或(pyrid-3-yl)dithiolan-4-ol)-基团取代的吲哚化合物是PAF的有效抑制剂，对于治疗与PAF相关的疾病包括过敏性休克、呼吸窘迫综合征、急性炎症、细胞免疫延迟、分娩、胎儿肺成熟和细胞分化是有用的。

  公开号：

  US05120749A1

文献信息

• 1H,3H-pyrrolo[1,2-c]thiazole derivatives having anti-allergic and
  申请人：Rhone-Poulenc Sante

  公开号：US04529728A1

  公开（公告）日：1985-07-16

  New compounds of the formula ##STR1## in which R.sub.1 and R.sub.2 =H or alkyl and (a) R=CN or alkylcarbonyl, or (b) R=CON(R.sub.3)R.sub.4, in which R.sub.3 =H and R.sub.4 =NH.sub.2, alkylamino, dialkylamino, phenylamino or diphenylamino; or R.sub.3 and R.sub.4 =H, alkyl (1 to 5 C) or substituted phenyl; or R.sub.3 =H and R.sub.4 =pyridyl or alkyl (1 to 5 C) substituted by COOH, NH.sub.2, alkylamino, dialkylamino, morpholino, piperidino, pyrrolidin-1-yl, piperazin-1-yl (optionally substituted by alkyl, pyridyl or optionally substituted phenyl or benzyl), optionally substituted phenyl, pyridyl or imidazolyl; or R.sub.3 and R.sub.4 form an imidazolyl radical or a 5-membered or 6-membered heterocycle which can contain an oxygen, sulphur or nitrogen atom and which is optionally substituted by alkyl, alkoxycarbonyl, hydroxyalkyl, aminoalkyl, alkylaminoalkyl, dialkylaminoalkyl, pyridyl, pyrimidinyl, pyrazinyl, optionally substituted phenyl or optionally substituted benzyl; or (c) R=--C(.dbd.NOH)NH.sub.2 or --C[.dbd.NN(R'R")NH.sub.2 ], in which R' and R"=alkyl, the said alkyl radicals and alkyl portions being straight-chain or branched-chain and, unless mentioned otherwise, containing 1 to 4 carbon atoms, and the substituted phenyl and benzyl radicals carrying a halogen atom or an alkyl, alkoxy, alkylthio, trifluoromethyl or dialkylamino radical, and their tautomeric forms, addition salts with acids and the metals salts and the addition salts with nitrogen bases, are useful anti-allergic and anti-inflammatory agents. A variety of methods of making them are described.

  具有通式##STR1##的新化合物，其中R1和R2=H或烷基，并且(a) R=CN或烷基羰基，或(b) R=CON(R3)R4，其中R3=H且R4=NH2、烷基氨基、二烷基氨基、苯基氨基或二苯基氨基；或R3和R4=H、烷基（1至5个碳）或取代的苯基；或R3=H且R4=吡啶基或被COOH、NH2、烷基氨基、二烷基氨基、吗啉基、哌啶基、吡咯烷-1-基、哌嗪-1-基（可选择性地被烷基、吡啶基或可选择性地被取代的苯基或苄基取代）、可选择性地被取代的苯基、吡啶基或咪唑基取代的烷基（1至5个碳）；或R3和R4形成咪唑基或含有氧、硫或氮原子的5元或6元杂环，该杂环可选择性地被烷基、烷氧羰基、羟基烷基、氨基烷基、烷基氨基烷基、二烷基氨基烷基、吡啶基、嘧啶基、吡嗪基、可选择性地被取代的苯基或可选择性地被取代的苄基取代；或(c) R=--C(.dbd.NOH)NH2或--C[.dbd.NN(R'R")NH2]，其中R'和R"=烷基，所述烷基基团和烷基部分为直链或支链，除非另有说明，含有1至4个碳原子，并且被取代的苯基和苄基基团带有卤素原子或烷基、烷氧基、烷硫基、三氟甲基或二烷基氨基基团，以及它们的互变异构形式、与酸的加成盐和金属盐以及与氮碱的加成盐，是有用的抗过敏和抗炎剂。描述了制备它们的各种方法。
• Benzoylphenyl pyridinylthiazolidine compounds as platelet activating
  申请人：Abbott Laboratories

  公开号：US05120751A1

  公开（公告）日：1992-06-09

  Benzoylphenyl derivatives of 2-(3-pyridinyl)-3-alkyl-4-thiazolidinecarboxamide, 2-(3-pyridinyl)-thiazolid-4-ylacetamide, 2-(3-pyridinyl)-4-dithiolanecarboxamide or 2-(3-pyridinyl)dithiolan-4-yl] urea are potent inhibitors of PAF and are useful in the treatment of PAF-related disorders including anaphylactic shock, respiratory distress syndrome, acute inflammation, delayed cellular immunity, parturtition, fetal lung maturation, and cellular differentiation.

  苯甲酰苯基衍生物2-(3-吡啶基)-3-烷基-4-噻唑烷羧酰胺，2-(3-吡啶基)-噻唑-4-乙酰胺，2-(3-吡啶基)-4-二硫杂环己羧酰胺或2-(3-吡啶基)二硫杂环己-4-基] 尿素是PAF的强效抑制剂，并且在治疗PAF相关疾病中具有用途，包括过敏性休克、呼吸窘迫综合征、急性炎症、细胞免疫延迟、分娩、胎儿肺成熟和细胞分化。
• Condensed pyrrolo derivatives, process for their preparation and pharmaceutical compositions containing them
  申请人：YAMANOUCHI PHARMACEUTICAL CO. LTD.

  公开号：EP0425134A1

  公开（公告）日：1991-05-02

  A heterocyclic compound of the formula (I): and a pharmacologically acceptable salt thereof which have platelet activating factor (PAF) antagonizing activity are disclosed.

  公开了一种具有血小板活化因子（PAF）拮抗活性的化学式（I）的杂环化合物及其药理学上可接受的盐。
• Pyridylthiazolidine carboxamide derivatives and their intermediates and
  申请人：Yamanouchi Pharmaceutical Co., Ltd.

  公开号：US04948795A1

  公开（公告）日：1990-08-14

  This invention provides pyridylthiazolidine carboxamide derivative shown by general formula (I) and pharmaceutically acceptable salts thereof: ##STR1## wherein A.sup.1 is a single bond, carbonyl group or lower alkylene group which may include a carbonyl group and R.sup.1 is a heterocyclic ring which may be substituted with a lower alkyl group and further provides N-substituted piperazine derivatives useful as intermediates for preparing said compounds (I).

  本发明提供了一种由通式（I）表示的吡啶基噻唑烷羧酰胺衍生物及其药学上可接受的盐：##STR1## 其中A.sup.1是单键，羰基或较低的含有羰基的烷基，R.sup.1是杂环环，可以用较低的烷基基团取代，还提供了N-取代哌嗪衍生物，用于制备所述化合物（I）的中间体。
• N-substituted piperizine derivatives
  申请人：Yamanouchi Pharmaceutical Co., Ltd.

  公开号：US05144035A1

  公开（公告）日：1992-09-01

  This invention provides pyridylthiazolidine carboxamide derivative shown by general formula (I) and pharmaceutically acceptable salts thereof: ##STR1## wherein A.sup.1 is a single bond, carbonyl group or lower alkylene group which may include a carbonyl group and R.sup.1 is a heterocyclic ring which may be substituted with a lower alkyl group and further provides N-substituted piperazine derivatives useful as intermediates for preparing said compounds (I).

  该发明提供了一种由通式（I）所示的吡啶基噻唑烷羧酰胺衍生物及其药学上可接受的盐：##STR1##其中，A.sup.1是单键，羰基或较低的含有羰基的烷基，R.sup.1是杂环环，可以用较低的烷基取代，并且进一步提供了用于制备所述化合物（I）的中间体的N-取代哌嗪衍生物。