tetraethyl 2,2'-dithiodisuccinate | 2090-25-7

• 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
• 英文名称: tetraethyl 2,2'-dithiodisuccinate
• 英文别名: Tetraethyl-dithiodisuccinat；tetraethyl dithiomalate；Tetraethyl Dithiodisuccinate (TDDS)；diethyl 2-[(1,4-diethoxy-1,4-dioxobutan-2-yl)disulfanyl]butanedioate
• CAS: 2090-25-7
• 化学式: C₁₆H₂₆O₈S₂
• 分子量: 410.51
• InChiKey: WGYLQNYATPZUIZ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.9
• 重原子数：
  26
• 可旋转键数：
  17
• 环数：
  0.0
• sp3杂化的碳原子比例：
  0.75
• 拓扑面积：
  156
• 氢给体数：
  0
• 氢受体数：
  10

反应信息

• 作为反应物：
  描述：

  tetraethyl 2,2'-dithiodisuccinate 、 亚磷酸三乙酯 生成 diethoxyphosphorylsulfanyl-succinic acid diethyl ester
  参考文献：
  名称：

  Synthesis of O,O-Dimethyl S-(1,2-Dicarbethoxy)ethyl Phosphorothioate (Maloxon) and Related Compounds from Trialkyl Phosphites and Organic Disulfides

  摘要：

  DOI：

  10.1021/jo01015a028
• 作为产物：
  描述：

  2-巯基丁二酸二乙酯 在 盐酸 双氧水 作用下， 以 水 为溶剂， 反应 16.0h， 生成 tetraethyl 2,2'-dithiodisuccinate
  参考文献：
  名称：

  Process for Preparing Malathion for Pharmaceutical Use

  摘要：

  本发明提供了一种制备高纯度马拉硫磷的工艺，其具有较低水平的有毒杂质。此外，通过本发明的工艺制备的马拉硫磷具有良好的储存稳定性。例如，马拉硫磷中的有毒杂质水平，如异马拉硫磷、O,O,S-三甲基磷二硫代酸酯（MeOOSPS）、O,O,S-三甲基磷硫代酸酯（MeOOSPO）、O,S,S-三甲基磷二硫代酸酯（MeOSSPO）、马拉氧酮、异马拉硫磷、富马酸二乙酯、甲基马拉硫磷、二甲基马拉硫磷、O,O-甲基、乙基-S-(1,2-二羧乙氧基)乙基磷二硫代酸酯均低于任何其他可能用于药用目的的商业马拉硫磷制剂。

  公开号：

  US20070010496A1

文献信息

• Process for Preparing Malathion for Pharmaceutical Use
  申请人：Gutman Daniella

  公开号：US20070010496A1

  公开（公告）日：2007-01-11

  The present invention provides a process for preparing a highly pure form of malathion having a reduced level of toxic impurities. In addition, the malathion prepared by the process of this invention is storage stable. The level of toxic impurities in the malathion, e.g., isomalathion, O,O,S-trimethyl phosphorodithioate (MeOOSPS), O,O,S-trimethyl phosphorothioate (MeOOSPO), O,S,S-trimethyl phosphorodithioate (MeOSSPO), malaoxon, isomalathion, diethyl fumarate, methyl malathion, dimethyl malathion, O,O-methyl,ethyl-S-(1,2-dicarboethoxy)ethyl-phosphorodithioate are lower than that of any other commercial preparation of malathion that may be used for pharmaceutical purposes.

  本发明提供了一种制备高纯度马拉硫磷的工艺，其具有较低水平的有毒杂质。此外，通过本发明的工艺制备的马拉硫磷具有良好的储存稳定性。例如，马拉硫磷中的有毒杂质水平，如异马拉硫磷、O,O,S-三甲基磷二硫代酸酯（MeOOSPS）、O,O,S-三甲基磷硫代酸酯（MeOOSPO）、O,S,S-三甲基磷二硫代酸酯（MeOSSPO）、马拉氧酮、异马拉硫磷、富马酸二乙酯、甲基马拉硫磷、二甲基马拉硫磷、O,O-甲基、乙基-S-(1,2-二羧乙氧基)乙基磷二硫代酸酯均低于任何其他可能用于药用目的的商业马拉硫磷制剂。
• [EN] PROCESS FOR THE PREPARATION OF MALATHION AND ITS INTERMEDIATE<br/>[FR] PROCÉDÉ DE FABRICATION DE MALATHION ET DE SON INTERMÉDIAIRE
  申请人：SUVEN LIFE SCIENCES LTD

  公开号：WO2009007998A1

  公开（公告）日：2009-01-15

  The present invention relates to the improved process for the preparation of highly pure form of S-[1,2-(dicarbethoxy)-ethyl]O,O-dimethyl phosphorodithioate having formula (I). The compound of formula (I) has adopted name 'Malathion'. The present invention also relates to the novel process of preparing intermediate O,O- dimethyldithiophosphoric acid of formula (II), which is useful in the preparation of Malathion. The Malathion prepared by the process of this invention is highly storage stable and toxic impurities are much lower than any other commercial preparation available for the pharmaceutical purpose.

  本发明涉及改进的工艺，用于制备具有化学式(I)的高纯度S-[1,2-(二甲氧羰基)-乙基] O,O-二甲基磷硫二酸酯。化合物化学式(I)的通用名称为“马拉硫磷”。本发明还涉及制备中间体化学式(II)的新工艺，该中间体在制备马拉硫磷时非常有用。通过本发明的工艺制备的马拉硫磷具有高度的贮存稳定性，毒性杂质比任何其他用于药用目的的商业制剂都要低。
• PROCESS FOR PREPARING MALATHION FOR PHARMACEUTICAL USE
  申请人：Gutman Daniella

  公开号：US20090124823A1

  公开（公告）日：2009-05-14

  The present invention provides a process for preparing a highly pure form of malathion having a reduced level of toxic impurities. In addition, the malathion prepared by the process of this invention is storage stable. The level of toxic impurities in the malathion, e.g., isomalathion, O,O,S-trimethyl phosphorodithioate (MeOOSPS), O,O,S-trimethyl phosphorothioate (MeOOSPO), O,S,S-trimethyl phosphorodithioate (MeOSSPO), malaoxon, isomalathion, diethyl fumarate, methyl malathion, dimethyl malathion, O,O-methyl,ethyl-S-(1,2-dicarboethoxy)ethyl-phosphorodithioate are lower than that of any other commercial preparation of malathion that may be used for pharmaceutical purposes.

  本发明提供了一种制备高纯度马拉硫磷的方法，该方法降低了有毒杂质的含量。此外，本发明制备的马拉硫磷具有良好的储存稳定性。马拉硫磷中的有毒杂质含量，例如异马拉硫磷、O,O,S-三甲基磷二硫代酸酯（MeOOSPS）、O,O,S-三甲基磷酸酯（MeOOSPO）、O,S,S-三甲基磷二硫代酸酯（MeOSSPO）、马拉氧（malaoxon）、异马拉硫磷、己二酸二乙酯（diethyl fumarate）、甲基马拉硫磷（methyl malathion）、二甲基马拉硫磷（dimethyl malathion）、O,O-甲基、乙基-S-(1,2-二羧乙酸乙酯)磷二硫代酸酯的含量低于任何其他可用于制药目的的商业马拉硫磷制剂。
• TOPICAL GEL FORMULATION COMPRISING ORGANOPHOSPHATE INSECTICIDE AND PREPARATION THEREOF
  申请人：Goyal Sandhya

  公开号：US20120053153A1

  公开（公告）日：2012-03-01

  The present invention provides a topical gel pharmaceutical formulation of insecticide suitable for treating an ectoparasite in a mammal, comprising: a) about 0.1-10% by weight of an insecticide; b) at least about 75% by weight of an organic solvent selected from the group consisting of a lower alkyl alcohol, a ketone, a glycol and a mixture thereof, wherein the organic solvent contains at least about 40% by weight of the lower alkyl alcohol; and c) at least one polymer selected from the group consisting of a cellulosic polymer, acrylates, methacrylates, and polyvinyl pyrrolidone. The present gel pharmaceutical formulation preferably contains malathion and optionally contains isopropyl myristate. The present invention further provides a process of preparing as well as a method of treating ectoparasites in a mammal using the same.

  本发明提供了一种适用于治疗哺乳动物体内寄生虫的局部凝胶制剂，包括：a）约0.1-10％的杀虫剂重量；b）至少约75％的有机溶剂，所述有机溶剂选自较低的烷基醇，酮，乙二醇和其混合物组成的群体，其中所述有机溶剂含有至少约40％的较低的烷基醇重量；c）至少一种聚合物，所述聚合物选自纤维素聚合物，丙烯酸酯，甲基丙烯酸酯和聚乙烯吡咯烷酮组成的群体。本凝胶制剂首选含有马拉硫磷，可选择含异丙酸肉豆蔻酸酯。本发明还提供了一种制备方法以及使用该制剂治疗哺乳动物体内寄生虫的方法。
• Topical gel formulation comprising organophosphate insecticide and its preparation thereof
  申请人：Goyal Sandhya

  公开号：US20060084632A1

  公开（公告）日：2006-04-20

  The present invention provides a topical gel pharmaceutical formulation of insecticide suitable for treating an ectoparasite in a mammal, comprising: a) about 0.1-10% by weight of an insecticide; b) at least about 75% by weight of an organic solvent selected from the group consisting of a lower alkyl alcohol, a ketone, a glycol and a mixture thereof, wherein the organic solvent contains at least about 40% by weight of the lower alkyl alcohol; and c) at least one polymer selected from the group consisting of a cellulosic polymer, acrylates, methacrylates, and polyvinyl pyrrolidone. The present gel pharmaceutical formulation preferably contains malathion and optionally contains isopropyl myristate. The present invention further provides a process of preparing as well as a method of treating ectoparasites in a mammal using the same.

  本发明提供了一种适用于治疗哺乳动物体外寄生虫的杀虫剂局部凝胶药物制剂，包括： a) 约 0.1-10% (重量)的杀虫剂；b) 至少约 75% (重量)的有机溶剂，该有机溶剂选自由低级烷基醇、酮、乙二醇及其混合物组成的组，其中有机溶剂含有至少约 40% (重量)的低级烷基醇；和 c) 至少一种聚合物，该聚合物选自由纤维素聚合物、丙烯酸酯、甲基丙烯酸酯和聚乙烯吡咯烷酮组成的组。本发明的凝胶药物制剂最好含有马拉硫磷，并可选择含有肉豆蔻酸异丙酯。本发明进一步提供了一种制备方法以及使用本发明治疗哺乳动物体外寄生虫的方法。