2-methylpyridinium methanesulfonate

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡啶及其衍生物
• 英文名称: 2-methylpyridinium methanesulfonate
• 英文别名: alfa-picolinium methanesulfonate；Methanesulfonic acid;2-methylpyridine；methanesulfonic acid;2-methylpyridine
• 化学式: CH₄O₃S*C₆H₇N
• 分子量: 189.235
• InChiKey: GXWXBVSXQWXEHX-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.03
• 重原子数：
  12
• 可旋转键数：
  0
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.29
• 拓扑面积：
  79.7
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  环硫乙烷 、 2-methylpyridinium methanesulfonate 在 甲烷磺酸 作用下， 以 碳酸甲丙酯 为溶剂， 以2.13 g (85%)的产率得到1-(2-mercaptoethyl)-2-methylpyridinium methanesulfonate
  参考文献：
  名称：

  Carbapenem antibiotics

  摘要：

  本发明涉及一种新颖的碳青霉烯衍生物，其特征在于具有公式##STR1##中的2-取代基，其中A代表环戊烯基、环己烯基或C.sub.2-C.sub.6烷基，可选择地取代一个或多个C.sub.1-C.sub.4烷基，以及##STR2##代表季铵化的含氮芳香杂环。这些衍生物可用作有效的抗菌剂。还公开了制备这些衍生物的方法以及在这些方法中使用的新颖中间体。

  公开号：

  US04552696A1

文献信息

• [EN] IMPROVED PROCESS FOR THE PREPARATION OF BIOLOGICALLY ACTIVE TETRAHYDROBENZTHIAZOLE DERIVATIVE<br/>[FR] PROCEDE AMELIORE DE PREPARATION D'UN DERIVE DE TETRAHYDROBENZOTHIAZOLE BIOLOGIQUEMENT ACTIF
  申请人：ALEMBIC LTD

  公开号：WO2006003677A1

  公开（公告）日：2006-01-12

  Improved process for the preparation of the intermediate compound of formula II for formation pramipezole of formula (I) as well as the biological active tetrahydrobenzothiazole compound of formula (I) and/or its pharmaceutically acceptable salts or solvates.

  改进的工艺用于制备式(I)的前体化合物的中间化合物II，以及式(I)的前体pramipezole的生物活性四氢苯并噻唑化合物和/或其药用可接受的盐或溶剂。
• [EN] ORAL PHARMACEUTICAL COMPOSITIONS CONTAINING TAXANES AND METHODS OF TREATMENT EMPLOYING THE SAME<br/>[FR] COMPOSITIONS PHARMACEUTIQUES ORALES CONTENANT DES TAXANES ET METHODES DE TRAITEMENT DANS LESQUELLES LESDITES COMPOSITIONS SONT UTILISEES
  申请人：BAKER NORTON PHARMA

  公开号：WO2000078247A1

  公开（公告）日：2000-12-28

  Pharmaceutical compositions for oral administration to mammalian subjects comprise a taxane or taxane derivative (e.g., paclitaxel or docetaxel) as active ingredient and a vehicle comprising at least 30 % by weight of a carrier for the taxane, said carrier having an HLB value of at least about 10. The compositions may also comprise 0 - 70 % of a viscosity-reducing co-solubilizer. The compositions may be incorporated into conventional oral pharmaceutical dosage forms, or can be in the form of a two-part medicament wherein the first part includes the taxane in a solubilizing vehicle and the second part comprises a carrier for the taxane to promote oral absorption. Methods of treatment of taxane- responsive disease conditions employing the novel compositions are also disclosed, whereby the compositions can be administered alone or in association with an oral bioavailability enhancing agent.

  用于哺乳动物主体口服的制药组合物包括紫杉烷或紫杉烷衍生物（例如紫杉醇或多西他赛）作为活性成分和载体，所述载体的重量至少为30％，其HLB值至少约为10。该组合物还可以包含0-70％的减粘共溶剂。该组合物可以被纳入传统的口服药物剂量形式中，或者可以是双部分药物的形式，其中第一部分包括溶解剂载体中的紫杉烷，第二部分包括载体以促进口服吸收。还公开了使用这种新型组合物治疗紫杉烷敏感疾病状况的治疗方法，其中可以单独或与口服生物利用度增强剂联合使用该组合物。
• Process for the preparation of biologically active tetrahydrobenzthiazole derivative
  申请人：Mistry N. Dhiren

  公开号：US20070123573A1

  公开（公告）日：2007-05-31

  Improved process for the preparation of the intermediate compound of formula II for formation of biological active tetrahydrobenzothiazole compound of formula (I) as well as the biological active tetrahydrobenzothiazole compound of formula (I) and/or its pharmaceutically acceptable salts or solvates. The process comprises reacting 4-amino cyclohexanol of formula (III) or its acid addition salts with phthalic anhydride in presence of acid catalyst and their salts, in polar aprotic solvent or its mixture with organic solvent, capable of removing water azeotropically to give 4-(phthalimido)-cyclohexanol of formula (IV); oxidizing 4-(phthalimido)-cyclohexanol of formula (IV) to give 4-(phthalimido)-cyclohexanone of formula (V); brominating 4-(phthalimido)-cyclohexanone of formula (V) with brominating agent in organic solvent in presence of Lewis acid catalyst to prepare 2-bromo-4-(phthalimido)-cyclohexanone of formula (VI); treating 2-bromo-4-(phthalimido)-cyclohexanone of formula (VI) with thiourea in organic solvent in presence of base to give 2-amino-6-phthalimido-4,5,6,7-tetrahydro benzothiazol of formula (VII); reacting compound of formula (VII) with hydrazine hydrate and base in polar solvent to give racemic 2,6-diamino-4,5,6,7-tetrahydro-1,3-benzothiazole of formula (VIII); resolving racemic 2,6-diamino-4,5,6,7-tetrahydro-1,3-benzothiazole of formula (VIII) to prepare (6S)-2,6-diamino-4,5,6,7-tetrahydro-1,3-benzothiazole of formula (II). To form the compound of Formula I and if desired its salts/solvates the above process is carried out with further steps of coupling (6S)-2,6-dimino-4,5,6,7-tetrahydro-1,3-benzothiazole of formula (II) with propionaldehyde in presence of mineral acid in polar organic solvent and reducing agent to prepare (S)-(−)-2-Amino-6-(n-propylamino)-4,5,6,7-tetrahydrobenzothiazole of formula (I);and if desired converting (S)-(−)-2-Amino-6-(propylamino)-4,5,6,7-tetrahydrobenzothiazole to its pharmaceutically acceptable salts or solvates.

  改进的制备中间化合物II的工艺，用于制备生物活性四氢苯并噻唑化合物I，以及生物活性四氢苯并噻唑化合物I和/或其药学上可接受的盐或溶剂。该工艺包括在极性无水溶剂或其与有机溶剂的混合物中，与酸催化剂及其盐共同反应式III的4-氨基环己醇或其酸加成盐与邻苯二酸酐，能够共沸去除水的极性无水溶剂或其混合物，以给出式IV的4-(邻苯二酰亚胺)-环己醇；将式IV的4-(邻苯二酰亚胺)-环己醇氧化为式V的4-(邻苯二酰亚胺)-环己酮；在有机溶剂中，在路易斯酸催化剂的存在下，用溴化剂溴化式V的4-(邻苯二酰亚胺)-环己酮，以制备式VI的2-溴-4-(邻苯二酰亚胺)-环己酮；在碱的存在下，在有机溶剂中用硫脲处理式VI的2-溴-4-(邻苯二酰亚胺)-环己酮，以给出式VII的2-氨基-6-邻苯二酰亚胺-4,5,6,7-四氢苯并噻唑；在极性溶剂中，用肼水合物和碱反应式VII的化合物，以给出式VIII的外消旋2,6-二氨基-4,5,6,7-四氢-1,3-苯并噻唑；分离外消旋2,6-二氨基-4,5,6,7-四氢-1,3-苯并噻唑，制备式II的(6S)-2,6-二氨基-4,5,6,7-四氢-1,3-苯并噻唑。为了形成式I的化合物，如果需要其盐/溶剂，以上工艺还需进行以下步骤：在极性有机溶剂和还原剂的存在下，将(6S)-2,6-二氨基-4,5,6,7-四氢-1,3-苯并噻唑II与丙醛在矿物酸的存在下偶联，以制备式I的(S)-(−)-2-氨基-6-(n-丙基氨基)-4,5,6,7-四氢苯并噻唑；如果需要，将(S)-(−)-2-氨基-6-(n-丙基氨基)-4,5,6,7-四氢苯并噻唑转化为其药学上可接受的盐或溶剂。
• Oral pharmaceutical compositions containing taxanes and methods for treatment employing the same
  申请人：IVAX Research, Inc.

  公开号：EP1479382A1

  公开（公告）日：2004-11-24

  Pharmaceutical compositions for oral administration to mammalian subjects comprise a taxane or taxane derivative (e.g. paclitaxel or docetaxel) as active ingredient and a vehicle comprising at least 30% by weight of a carrier for the taxane, said carrier having an HLB value of at least about 10. The compositions may also comprise 0 - 70% of a viscosity-reducing co-solubilizer. The compositions may be incorporated into conventional oral pharmaceutical dosage forms, or can be in the form of a two-part medicament wherein the first part includes the taxane in a solubilizing vehicle and the second part comprises a carrier for the taxane to promote oral absorption. Methods of treatment of taxane-responsive disease conditions employing the novel compositions are also disclosed, whereby the compositions can be administered alone or in association with an oral bioavailability enhancing agent.

  用于哺乳动物口服给药的药物组合物包括作为活性成分的紫杉烷或紫杉烷衍生物（如紫杉醇或多西他赛），以及由至少 30% （按重量计）的紫杉烷载体组成的载体，所述载体的 HLB 值至少约为 10。组合物还可包含 0 - 70% 的降粘助溶剂。组合物可以加入常规口服药物剂型中，也可以是两部分药物的形式，其中第一部分包括增溶载体中的紫杉烷，第二部分包括促进口服吸收的紫杉烷载体。此外，还公开了使用新型组合物治疗紫杉烷反应性疾病的方法，其中组合物可单独给药，也可与口服生物利用度增强剂联合给药。
• Method, compositions and kits for increasing the oral bioavailability of pharmaceutical agents
  申请人：Ivax Research, Inc.

  公开号：EP1634607A2

  公开（公告）日：2006-03-15

  A method of increasing the bioavailability upon oral administration of a pharmacologically active target agent, particularly an antitumor or antineoplastic agent which exhibits poor or inconsistent oral bioavailability (e.g., paclitaxel, docetaxel or etoposide), comprises the oral co-administration to a mammalian patient of the target agent and an oral bioavailability-enhancing agent (e.g., cyclosporin A, cyclosporin D, cyclosporin F or ketoconazole). The enhancing agent may be administered orally from 0.5-24 hrs. prior to the oral administration of one or more doses of the target agent, substantially simultaneously with the target agent or both prior to and substantially simultaneously with the target agent. A method of treating mammalian patients suffering from diseases responsive to target agents with poor oral bioavailability, as well as oral dosage forms containing such target agents, combination oral dosage forms containing bioavailability-enhancing agents and target agents kits containing enhancing and target agent dosage forms and dosing information for the co-administration of the same are also disclosed.

  一种提高药理活性靶向药物口服后的生物利用度的方法，特别是口服生物利用度较差或不稳定的抗肿瘤或抗肿瘤药物（如紫杉醇、多西他赛或依托泊苷），包括向哺乳动物患者口服靶向药物和口服生物利用度增强剂（如环孢素A、环孢素D、环孢素F或酮康唑）。增强剂可在口服一种或多种剂量的靶向药之前 0.5-24 小时口服，或与靶向药基本同时口服，或在口服靶向药之前和与靶向药基本同时口服。此外，还公开了一种治疗哺乳动物患者对口服生物利用度较低的靶向制剂有反应的疾病的方法，以及含有此类靶向制剂的口服剂型、含有生物利用度增强剂和靶向制剂的组合口服剂型、含有增强剂和靶向制剂剂型的试剂盒以及联合给药的剂量信息。