Invention Grant
US07718812B2 Process for the preparation of 2-(6-substituted-1,3-dioxane-4-yl) acetic acid derivates 有权
2-(6-取代-1,3-二恶烷-4-基)乙酸衍生物的制备方法

  • Patent Title: Process for the preparation of 2-(6-substituted-1,3-dioxane-4-yl) acetic acid derivates
  • Patent Title (中): 2-(6-取代-1,3-二恶烷-4-基)乙酸衍生物的制备方法
  • Application No.: US10501250
    Application Date: 2002-12-09
  • Publication No.: US07718812B2
    Publication Date: 2010-05-18
  • Inventor: Robert Patrick Hof
  • Applicant: Robert Patrick Hof
  • Applicant Address: GB London
  • Assignee: AstraZeneca UK Limited
  • Current Assignee: AstraZeneca UK Limited
  • Current Assignee Address: GB London
  • Agency: Morgan, Lewis & Bockius LLP
  • Priority: EP01000794 20011227
  • International Application: PCT/NL02/00876 WO 20021209
  • International Announcement: WO03/059901 WO 20030724
  • Main IPC: C07D319/06
  • IPC: C07D319/06
Process for the preparation of 2-(6-substituted-1,3-dioxane-4-yl) acetic acid derivates
Abstract:
The invention relates to a process for the conversion of group X in a 2-(6-substituted)-1,3-dioxane-4yl) acetic acid derivative according to formula 2 into a group OY in the presence of a phase transfer catalyst and an oxylating agent, by using as a phase transfer catalyst a quarternary phosphonium ion and by using as an oxylating agent an OY-ion. X stands for a halogen and R1, R2 and R3 are each independently a C1–4 alkylgroup or R1 and R2 together with the C-atom to which they are bound form a 5- or 6-membered cycloalkyl; Y stands for RA-CO— or for RB—SO2- with RA, RB are chosen from the group of alkyl or aryl with 1–12 C-atoms.
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