Global Patent Index - EP 1831236 A4

EP 1831236 A4 20131120 - METHOD FOR THE PREPARATION OF 2'-DEOXY-2',2'-DIFLUOROCYTIDINE

Title (en)

METHOD FOR THE PREPARATION OF 2'-DEOXY-2',2'-DIFLUOROCYTIDINE

Title (de)

VERFAHREN ZUR HERSTELLUNG VON 2'-DEOXY-2',2'-DIFLUOROCYTIDIN

Title (fr)

METHODE SERVANT A PREPARER 2'-DEOXY-2',2'-DIFLUOROCYTIDINE

Publication

EP 1831236 A4 20131120 (EN)

Application

EP 05823850 A 20051229

Priority

  • KR 2005004633 W 20051229
  • KR 20040116316 A 20041230
  • KR 2005001954 W 20050623

Abstract (en)

[origin: WO2006071090A1] This invention relates to an improved method for stereoselectively preparing 2¢¥-deoxy-2¢¥,2¢¥-difluorocytidine of formula (I), which comprises the steps of reacting a 1-halo ribofuranose compound of formula (III) with a nucleobase of formula (IV) in a solvent to obtain a nucleoside of formula (II) with removing the silyl halide of formula (V) produced during the reaction; and deprotecting the nucleoside of formula (II) to obtain 2¢¥-deoxy-2¢¥,2¢¥-difluorocytidine of formula (I).

IPC 8 full level

C07H 19/04 (2006.01)

CPC (source: EP)

C07H 19/04 (2013.01)

Citation (search report)

  • [X] CN 1442420 A 20030917 - HANDESEN TECHNOLOGY CO LTD SHE [CN]
  • [XY] VORBRUEGGEN, HELMUT ET AL: "Synthesis of nucleosides", ORGANIC REACTIONS, 2000, (HOBOKEN, NJ, UNITED STATES), XP002713324
  • [IA] BARDOS, THOMAS J. ET AL: "Stereoselective synthesis of the anomeric 5-mercapto-2'-deoxyuridines and of some other anomeric 2-deoxy-D-erythropentonucleosides", TETRAHEDRON LETTERS, vol. 16, 1966, pages 1759 - 1764, XP002713325, ISSN: 0040-4039
  • [YA] KOTICK, MICHAEL P. ET AL: "Synthesis of 5-s-substituted 2'-deoxyuridines. Study of the factors influencing the stereoselectivity of the silyl modification of the Hilbert-Johnson reaction", JOURNAL OF ORGANIC CHEMISTRY, vol. 34, no. 12, 1969, pages 3806 - 3813, XP002713326, ISSN: 0022-3263
  • See references of WO 2006071090A1

Designated contracting state (EPC)

AT BE BG CH CY CZ DE DK EE ES FI FR GB GR HU IE IS IT LI LT LU LV MC NL PL PT RO SE SI SK TR

DOCDB simple family (publication)

WO 2006071090 A1 20060706; AU 2005320374 A1 20060706; AU 2005320374 B2 20090108; BR PI0514718 A 20080701; CN 101010329 A 20070801; CN 101010329 B 20110608; EP 1831236 A1 20070912; EP 1831236 A4 20131120; NO 20070865 L 20070424

DOCDB simple family (application)

KR 2005004633 W 20051229; AU 2005320374 A 20051229; BR PI0514718 A 20051229; CN 200580029086 A 20051229; EP 05823850 A 20051229; NO 20070865 A 20070215