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    • 3. 发明专利
    • Production of ketopantolactone
    • 生产酮二醇
    • JPS59106479A
    • 1984-06-20
    • JP21583082
    • 1982-12-09
    • Seitetsu Kagaku Co Ltd
    • KAWAMURA MASAOAKUTSU SEIICHITAKAHASHI MASAHIDEOONISHI JIICHI
    • C07D307/60
    • PURPOSE: Pantolactone is oxidized with chlorine in an organic solvent in the presence of bromine and water to produce the titled compound which is used as an intermediate of D-(-)-pantolactone used as a starting compound for pantethine in higy yield with reduction in by-product formation.
      CONSTITUTION: Pantolactone is combined with 0.98W0.1mole of chlorine, 0.02W 0.9mole of bromine and 10W100% of water based on the pantolactone and they are refluxed, preferably in the presence of an organic solvent such as carbon tetrachloride, at the boiling point of the solvent to give the objective ketopantolactone. The use of a mixed system of Br
      2 and Cl
      2 can oxidize HBr formed as a by-product by bromine oxidation with chlorine to effect the reaction of 2HBr+Cl
      2 →2HCl+Br
      2 and the resultant Br
      2 is used again as the oxidizing agent.
      COPYRIGHT: (C)1984,JPO&Japio
    • 目的:在溴和水的存在下,用有机溶剂中的氯氧化内消旋酮,产生标题化合物,该化合物用作作为泛酸盐的起始化合物的D - ( - ) - 泛酸内酯的中间体,以高产率还原 副产品形成。 构成:根据泛酸内酯,将泛酸内酯与0.98-0.1摩尔氯,0.02-0.9摩尔溴和10-100%水混合,并优选在有机溶剂如四氯化碳的存在下回流 溶剂的沸点得到目标酮戊酸内酯。 使用Br2和Cl2的混合体系可以通过用溴氧化作为副产物氧化形成的HBr,以进行2HBr + Cl 2 2HCl + Br 2的反应,再次使用所得的Br 2作为氧化剂。
    • 9. 发明专利
    • Preparation of alpha-keto acid and/or its salt
    • 阿尔卡特酸和/或其盐的制备
    • JPS59164749A
    • 1984-09-17
    • JP3970183
    • 1983-03-09
    • Seitetsu Kagaku Co Ltd
    • KAWAMURA MASAOAKUTSU SEIICHITAKAHASHI MASAHIDEHATA HIROYUKIMORISHITA TSUYOSHINISHIMORI HIROKUNI
    • C07C59/185C07C51/00C07C51/09C07C51/373C07C59/205C07C59/21C07C59/76C07C67/00
    • PURPOSE: To prepare the titled compound useful industrially as pharmaceuticals, etc., economically, in high yield, by reacting an aldehyde with an oxalic acid ester in the presence of a metal alcoholate, and hydrolyzing the product with an alkali.
      CONSTITUTION: The objective compound of formula II is prepared by reacting the aldehyde of formula I (R
      1 and R
      2 are 1W18C alkyl, halogen-substituted alkyl, 3W8C cycloalkyl, or aromatic hydrocarbon group) with an oxalic acid ester of formula (COOR
      3 )
      2 (R
      3 is 1W5C alkyl) in the presence of a metal alcoholate of formula ROM (R is 1W18C alkyl; M is alkali metal or alkaline earth metal), preferably in a solvent such as methyl alcohol, dioxane, etc. at -70W +50°C, preferably at 8W12°C, hydrolyzing the reaction mixture with an alkali such as sodium hydroxide, and treating the product with a mineral acid. The molar ratio of the compound of formula I to the oxalic acid ester preferably 1.0W1.2.
      COPYRIGHT: (C)1984,JPO&Japio
    • 目的:在金属醇化物的存在下,通过使醛与草酸酯反应,并以碱的方式使产物水解,从经济上高效率地制备作为药物等在工业上有用的标题化合物。 结构式:式II的目的化合物是通过使式I的醛(R1和R2是1-18C烷基,卤素取代的烷基,3-8C环烷基或芳族烃基)与式(III)的草酸酯反应制备的, COOR3)2(R3为1-5C烷基)在式ROM的金属醇化物(R为1-18C烷基; M为碱金属或碱土金属)的存在下,优选在溶剂如甲醇,二恶烷, 在-70- + 50℃,优选在8-12℃,用碱如氢氧化钠水解反应混合物,并用无机酸处理该产物。 式I化合物与草酸酯的摩尔比优选为1.0-1.2。