Invention Grant
US08236946B2 Process for the preparation of 17-0-vinyl-triflates as intermediates 有权
制备17-0-乙烯基 - 三氟甲磺酸酯作为中间体的方法

  • Patent Title: Process for the preparation of 17-0-vinyl-triflates as intermediates
  • Patent Title (中): 制备17-0-乙烯基 - 三氟甲磺酸酯作为中间体的方法
  • Application No.: US11660792
    Application Date: 2005-08-23
  • Publication No.: US08236946B2
    Publication Date: 2012-08-07
  • Inventor: Paul S Bury
  • Applicant: Paul S Bury
  • Applicant Address: GB London
  • Assignee: BTG International Limited
  • Current Assignee: BTG International Limited
  • Current Assignee Address: GB London
  • Agency: Nixon & Vanderhye
  • Priority: GB0418900.7 20040824; GB0418901.5 20040824
  • International Application: PCT/GB2005/003283 WO 20050823
  • International Announcement: WO2006/021777 WO 20060302
  • Main IPC: C07J43/00
  • IPC: C07J43/00
Process for the preparation of 17-0-vinyl-triflates as intermediates
Abstract:
Process for the preparation of a compound of formula (I) as defined herein by (i) triflating a ketone of formula (II) as defined herein to form a triflate of formula (III) as defined herein and (ii) reacting the compound of the formula (III) to form a compound of the formula (I) or a pharmaceutically-acceptable salt thereof. The triflating step is conducted in the presence of a base comprising a tertiary or heterocyclic amine such that the pKa of the conjugate acid at 25° C. is within the range 5.21 to 12. The base is selected from pyridine, 2,6-lutidine, N-methylmorpholine, 1,4-diazabicyclo[2.2.2]octane (DABCO), trimethylamine, triethylamine, N,N-diisopropylethylamine (DIPEA), quinuclidine and 1,8-diazabicyclo[5.4.0]undec-7-ene (DBU).
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