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US09315525B2 Synthetic route for the preparation of α-amino boronic acid derivatives via substituted alk-1-ynes 有权
通过取代的alk-1-ynes制备α-氨基硼酸衍生物的合成路线

  • Patent Title: Synthetic route for the preparation of α-amino boronic acid derivatives via substituted alk-1-ynes
  • Patent Title (中): 通过取代的alk-1-ynes制备α-氨基硼酸衍生物的合成路线
  • Application No.: US13379181
    Application Date: 2010-06-18
  • Publication No.: US09315525B2
    Publication Date: 2016-04-19
  • Inventor: Ivana Gazic Smilovic , Zdenko Casar
  • Applicant: Ivana Gazic Smilovic , Zdenko Casar
  • Applicant Address: SI Ljubljana
  • Assignee: Lek Pharmaceuticals D.D.
  • Current Assignee: Lek Pharmaceuticals D.D.
  • Current Assignee Address: SI Ljubljana
  • Agency: Arent Fox LLP
  • Priority: EP09163227 20090619; EP09166475 20090727; EP09180099 20091221
  • International Application: PCT/EP2010/058666 WO 20100618
  • International Announcement: WO2010/146172 WO 20101223
  • Main IPC: C07F5/02
  • IPC: C07F5/02
Synthetic route for the preparation of α-amino boronic acid derivatives via substituted alk-1-ynes
Abstract:
A process for producing bortezomib N-(pyrazin-2-yl)carbonyl-L-phenylalanine-L-leucine boronic acid) comprising the step of deprotecting the compound of formula XII: to yield bortezomib.
Abstract(Chinese):

制备硼替佐米N-（吡嗪-2-基）羰基-L-苯丙氨酸-L-亮氨酸硼酸的方法，其包括使式XII化合物脱保护的步骤：产生硼替佐米。

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