1,1-bis(diethoxyphosphoryl)-1-chloroethane | 51346-83-9

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 有机膦酸及其衍生物
• 英文名称: 1,1-bis(diethoxyphosphoryl)-1-chloroethane
• 英文别名: tetraethyl 1-chloroethane-1,1-diphosphonate；1,1-Bis(diethoxyphosphinyl)-1-chloroethane；1-chloro-1,1-bis(diethoxyphosphoryl)ethane
• CAS: 51346-83-9
• 化学式: C₁₀H₂₃ClO₆P₂
• 分子量: 336.69
• InChiKey: MKRYRFXOENSIDS-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.2
• 重原子数：
  19
• 可旋转键数：
  10
• 环数：
  0.0
• sp3杂化的碳原子比例：
  1.0
• 拓扑面积：
  71.1
• 氢给体数：
  0
• 氢受体数：
  6

反应信息

• 作为产物：
  描述：

  diethyl 1,1-bis(diethoxyphosphoryl)ethyl phosphite 在 五氯化磷 作用下， 以60%的产率得到1,1-bis(diethoxyphosphoryl)-1-chloroethane
  参考文献：
  名称：

  Reaction in the ketophosphonate-triethylphosphite-diethylchlorophosphite ternary system

  摘要：

  DOI：

  10.1134/s1070363209040318

文献信息

• Halomethyl—metal compounds
  作者：Dietmar Seyferth、Robert S. Marmor

  DOI：10.1016/s0022-328x(00)95040-x

  日期：1973.10

  dichloromethylenediphosphonate gave the reagents LiCCl2P (O) (OEt)2 and [(EtO)2(O)P]2CClLi, respectively. The hydrolyses of these reagents, some coupling reactions with dimethyl sulfate, allyl bromide and trimethylchlorosilane and their use in the synthesis of chloroolefins are described.

  正丁基锂在THF中在低温下对三氯甲基膦酸二乙酯和四氯二氯亚甲基二膦酸酯的作用分别得到了试剂LiCCl 2 P（O）（OEt）2和[（EtO）2（O）P] 2 CClLi。描述了这些试剂的水解，与硫酸二甲酯，烯丙基溴和三甲基氯硅烷的一些偶联反应及其在合成氯烯烃中的用途。
• Methanediphosphonate derivative, its manufacturing process and its
  申请人：Toray Industries, Inc.

  公开号：US05527940A1

  公开（公告）日：1996-06-18

  The present invention relates to a methanediphosphonate derivative, its manufacturing process and pharmaceutical applications, that is represented with the following formula: ##STR1## (wherein, B is either hydrogen, an alkyl group, hydroxyl group, alkoxy group or amino group, D is either sulfur, oxygen, NH, alkyl-substituted N, CH.sub.2 or SCH.sub.2, X represents an alkyl group, alkyl group having a hetero atom as a substitution group, an aryl group or an acyl group, m represents an integer of 1 to 5, and R.sup.1, R.sup.2, R.sup.3 and R.sup.4 independently represent hydrogen, alkyl groups having 1 to 7 carbon atoms or pharmaceutically allowable cations). The compound of the present invention has excellent IL-1 inhibitory action, antioxidation action and bone resorption inhibitory action, and is useful as an antiinflammatory agent, antirheumatic, bone metabolic disease drug, autoimmune disease drug, osteoporosis drug and so forth.

  本发明涉及一种甲烷二膦酸盐衍生物及其制备方法和药物应用，其化学式如下：##STR1## （其中，B为氢、烷基、羟基、烷氧基或氨基；D为硫、氧、NH、烷基取代的N、CH.sub.2或SCH.sub.2；X表示烷基、含有杂原子的烷基、芳基或酰基；m表示1到5的整数；R.sup.1、R.sup.2、R.sup.3和R.sup.4独立地表示氢、具有1到7个碳原子的烷基或药用可允许的阳离子）。本发明的化合物具有出色的IL-1抑制作用、抗氧化作用和抑制骨吸收作用，可用作抗炎剂、抗风湿药、骨代谢疾病药、自身免疫病药、骨质疏松症药等。
• Pharmaceutical applications for methanediphosphonate derivative
  申请人：Toray Industries, Inc.

  公开号：US05683992A1

  公开（公告）日：1997-11-04

  The present invention relates to a methanediphosphonate derivative, its manufacturing process, and pharmaceutical applications, that is represented with the following formula: ##STR1## wherein, D is either sulfur, oxygen, NH, alkyl-substituted N, CH.sub.2, or SCH.sub.2, X represents an alkyl group, alkyl group having a hetero atom as a substitution group, an aryl group or an acyl group, m represents an integer of 1 to 5, and R.sup.1, R.sup.2, R.sup.3 and R.sup.4 independently represent hydrogen, alkyl groups having 1 to carbon atoms or pharmaceutically allowable cations. .function.The compounds of the present invention have excellent IL-1 inhibitory action, antioxidation action and bone resorption inhibitory action, and are useful as antiinflammatory agents, antirheumatic agents, bone metabolic disease drugs, autoimmune disease drugs, or osteoporosis drugs.

  本发明涉及一种甲烷二膦酸酯衍生物、其制造方法和药物应用，其化学式如下：##STR1## 其中，D 可为硫、氧、NH、烷基取代的 N、CH.sub.2 或 SCH.sub.2，X 代表烷基、带有杂原子的烷基取代基、芳基或酰基，m 为1到5的整数，R.sup.1、R.sup.2、R.sup.3 和 R.sup.4 分别代表氢、1到碳原子的烷基或药学上允许的阳离子。本发明的化合物具有出色的 IL-1 抑制作用、抗氧化作用和骨吸收抑制作用，可用作抗炎药、抗风湿药、骨代谢疾病药、自身免疫疾病药或骨质疏松症药物。
• METHANEDIPHOSPHONIC ACID DERIVATIVE, PRODUCTION THEREOF AND MEDICINAL USE THEREOF
  申请人：TORAY INDUSTRIES, INC.

  公开号：EP0594857A1

  公开（公告）日：1994-05-04

  A methanediphosphonic acid derivative represented by formulae (I) or (II), a process for producting the same, and a medicinal use thereof, wherein B represents hydrogen, alkyl, hydroxy, alkoxy or amino; D represents sulfur, oxygen, NH, alkyl-substituted nitrogen, CH₂ or SCH₂; X represents alkyl which may be substituted by a heteroatom, aryl or acyl; m represents an integer of 1 to 5; and R¹, R², R³ and R⁴ represent each independently hydrogen, C₁ to C₇, alkyl or a pharmacologically acceptable cation. The compound is excellent in IL-1 inhibition, antioxidant activity and bone resorption inhibition and useful for treating inflammation, rheumatism, bone metabolism disorder, autoimmune disease, osteoporosis, and so forth.

  一种由式(I)或(II)代表的甲烷二膦酸衍生物、制备该衍生物的工艺及其医药用途，其中 B 代表氢、烷基、羟基、烷氧基或氨基；D 代表硫、氧、NH、烷基取代的氮、CH₂或 SCH₂；X 代表可被杂原子、芳基或酰基取代的烷基；m 代表 1 至 5 的整数；以及 R¹、R²、R³ 和 R⁴ 各自独立地代表氢、C₁ 至 C₇、烷基或药理学上可接受的阳离子。该化合物具有优异的抑制 IL-1、抗氧化活性和抑制骨吸收的作用，可用于治疗炎症、风湿病、骨代谢紊乱、自身免疫性疾病、骨质疏松症等。
• US5527940A
  申请人：——

  公开号：US5527940A

  公开（公告）日：1996-06-18