ethyl phosphinate

• 分子结构分类: 有机化合物 - 有机氧化合物 - 有机含氧阴离子化合物
• 英文名称: ethyl phosphinate
• 英文别名: ethyl hypophosphite；EtOP(O)H2；(Phosphorosooxy)ethane；1-phosphorosooxyethane
• 化学式: C₂H₅O₂P
• 分子量: 92.0343
• InChiKey: ZMIRFCWMDNOYEN-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0
• 重原子数：
  5
• 可旋转键数：
  1
• 环数：
  0.0
• sp3杂化的碳原子比例：
  1.0
• 拓扑面积：
  26.3
• 氢给体数：
  0
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  ethyl phosphinate 以77%的产率得到
  参考文献：
  名称：

  NATCHEV, IVAN A., LIEBIGS ANN. CHEM.,(1988) N 9, C. 861-867

  摘要：

  DOI：
• 作为产物：
  描述：

  diethoxydimethylsilicate 在 次磷酸 作用下， 以 水 、 乙腈 为溶剂， 反应 2.0h， 生成 ethyl phosphinate
  参考文献：
  名称：

  P-取代的 5-和 6-元苯并-Phostams 的合成：2,3-Dihydro-1H-1,2-benzazaphosphole 2-Oxides 和 2,3-Tetrahydro-1H-1,2-benzazaphosphinine 2-Oxides

  摘要：

  开发了几种方法来制备磷取代的 5 和 6 元苯并磷酰胺。由硝基苯前体衍生的两性离子氨基次膦酸盐的碳二亚胺促进的环化以良好的产率完成了环化。或者，膦酰胺和溴苯前体之间的新型铜催化交叉偶联以中等至良好的产率产生杂环。比较了三种不同的方法来合成P-乙氧基取代的 5 元苯并磷酰胺。

  DOI：

  10.1021/acs.joc.1c01501

文献信息

• Facile P,N-heterocycle synthesis via tandem aminomethylation–cyclization of H-phosphinate building blocks
  作者：Clémence Queffélec、Jean-Luc Montchamp

  DOI：10.1039/b917428a

  日期：——

  Various heterocycles containing phosphorus and nitrogen are easily synthesized from readily available H-phosphinate building blocks. Aminomethylation of these H-phosphinates is followed by in situ cyclization through substitution or cross-coupling to produce novel heterocycles in moderate to good yields.

  含磷和氮的多种杂环化合物能够容易地从易得的H-膦酸酯砌块合成。对这些H-膦酸酯进行胺甲基化后，通过取代或交叉耦合进行原位环化，以中等至良好的产率得到新型杂环化合物。
• Phosphinate esters
  申请人：Ciba-Geigy Corporation

  公开号：US05488171A1

  公开（公告）日：1996-01-30

  A compound of formula ##STR1## where R.sup.1 and R.sup.2 are independently a C.sub.1 -C.sub.10 aliphatic radical, or R.sup.1 is a C.sub.1 -C.sub.10 aliphatic radical and R.sup.2 is a C.sub.6 -C.sub.10 aromatic radical, and R.sup.3 is a C.sub.1 -C.sub.8 aliphatic radical, a C.sub.3 -C.sub.8 cycloaliphatic radical, a C.sub.6 -C.sub.15 aromatic radical or a C.sub.7 -C.sub.13 araliphatic radical, provided that R.sup.3 is not methyl when R.sup.1 and R.sup.2 are each methyl, that R.sup.3 is not ethyl when R.sup.1 and R.sup.2 are each methyl and that R.sup.2 is not p-aminophenyl when R.sup.1 is methyl and R.sup.3 is ethyl.

  式为##STR1##的化合物，其中R.sup.1和R.sup.2分别是C.sub.1 -C.sub.10脂肪基，或者R.sup.1是C.sub.1 -C.sub.10脂肪基而R.sup.2是C.sub.6 -C.sub.10芳香基，而R.sup.3是C.sub.1 -C.sub.8脂肪基，C.sub.3 -C.sub.8环脂基，C.sub.6 -C.sub.15芳香基或C.sub.7 -C.sub.13芳基脂基，前提是当R.sup.1和R.sup.2分别为甲基时，R.sup.3不是甲基，当R.sup.1和R.sup.2分别为甲基时，R.sup.3不是乙基，当R.sup.1为甲基且R.sup.3为乙基时，R.sup.2不是对氨基苯基。
• Process for the preparation of derivatives of bis(amino-methyl)
  申请人：Hoechst Aktiengesellschaft

  公开号：US05510504A1

  公开（公告）日：1996-04-23

  A process for the preparation of .alpha.- or .alpha.,.alpha.'-substituted derivatives of the bis(aminomethyl)phosphinic acid of the formula I and their acid or basic salts, ##STR1## in which R.sup.1, R.sup.2 and R.sup.3 are defined as in the description, wherein a bis(aminomethyl)phosphinate is converted into the corresponding bisimine, which is alkylated by R.sup.2 and R.sup.3 in the .alpha.- and/or .alpha.,.alpha.'-position after reaction with a base, and is converted into a compound of the formula I by subsequent treatment with an acid.

  一种制备公式I的双(氨甲基)膦酸的α-或α，α'-取代衍生物及其酸性或碱性盐的方法，其中R.sup.1、R.sup.2和R.sup.3的定义如描述中所述，其中双(氨甲基)膦酸酯被转化为相应的双亚胺，与碱反应后在α-和/或α，α'-位置被R.sup.2和R.sup.3烷基化，并通过随后用酸处理转化为公式I的化合物。
• Method of synthesizing an organophosphorus compound
  申请人：Novartis Corp.

  公开号：US05693799A1

  公开（公告）日：1997-12-02

  A compound of formula ##STR1## where R.sup.1 and R.sup.2 are independently a C.sub.1 -C.sub.10 aliphatic radical, or R.sup.1 is a C.sub.1 -C.sub.10 aliphatic radical and R.sup.2 is a C.sub.6 -C.sub.10 aromatic radical, and R.sup.3 is a C.sub.1 -C.sub.8 aliphatic radical, a C.sub.3 -C.sub.8 cycloaliphatic radical, a C.sub.6 -C.sub.15 aromatic radical or a C.sub.7 -C.sub.13 araliphatic radical, provided that R.sup.3 is not methyl when R.sup.1 and R.sup.2 are each methyl, that R.sup.3 is not ethyl when R.sup.1 and R.sup.2 are each methyl and that R.sup.2 is not p-aminophenyl when R.sup.1 is methyl and R.sup.3 is ethyl with an organic compound having at least one group reactive with a P--H bond.

  一种化合物的化学式为##STR1##其中R.sup.1和R.sup.2分别为C.sub.1-C.sub.10脂肪基，或R.sup.1为C.sub.1-C.sub.10脂肪基，而R.sup.2为C.sub.6-C.sub.10芳香基，R.sup.3为C.sub.1-C.sub.8脂肪基，C.sub.3-C.sub.8环状脂肪基，C.sub.6-C.sub.15芳香基或C.sub.7-C.sub.13芳基脂肪基，但当R.sup.1和R.sup.2分别为甲基时，R.sup.3不是甲基，当R.sup.1和R.sup.2分别为甲基且R.sup.3为乙基时，R.sup.3不是乙基，当R.sup.1为甲基且R.sup.3为乙基时，R.sup.2不是对氨基苯基，该化合物至少含有一种与P-H键反应的基团。
• Azole compounds
  申请人：Takeda Pharmaceutical Company Limited

  公开号：US07183276B2

  公开（公告）日：2007-02-27

  The present invention provides a compound represented by the formula (I) wherein R1 is a hydrogen atom, a halogen atom, an optionally substituted hydrocarbon group, an optionally substituted heterocyclic group, an optionally substituted hydroxy group, an optionally substituted thiol group or an optionally substituted amino group, A is an optionally substituted cyclic amino group or —NR2—W—D wherein R2 is a hydrogen atom or an alkyl group, W is a bond or a divalent acyclic hydrocarbon group, and D is an optionally substituted cyclic group, an optionally substituted amino group or an optionally substituted acyl group, B is an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group, X is an oxygen atom, a sulfur atom or an optionally substituted nitrogen atom, and Y is a bond or a divalent acyclic hydrocarbon group, or a salt thereof, which is useful for the prophylaxis or treatment of diabetic neuropathy and the like.

  本发明提供了一种化合物，其表示为式（I），其中R1为氢原子，卤素原子，可选取代的碳氢基团，可选取代的杂环基团，可选取代的羟基，可选取代的硫醇基或可选取代的氨基；A为可选取代的环状氨基基团或-NR2-W-D，其中R2为氢原子或烷基团，W为键或二价非环烷基团，D为可选取代的环状基团，可选取代的氨基或可选取代的酰基；B为可选取代的碳氢基团或可选取代的杂环基团；X为氧原子，硫原子或可选取代的氮原子；Y为键或二价非环烷基团。该化合物或其盐对于预防或治疗糖尿病性神经病变等疾病有用。