PROCESS FOR THE PRODUCTION OF PURINE DERIVATIVES

Title:

PROCESS FOR THE PRODUCTION OF PURINE DERIVATIVES

Document Type and Number:

WIPO Patent Application WO1999051604

Kind Code:

A3

Abstract:

The invention provides a method of rearranging a compound of formula (I), wherein R and R' are selected independently from hydrogen and C1-12alkyl; and R1 and R2 are selected independently from hydrogen, hydroxy, halo, C1-12alkyl- or aryl carbonate, amino, mono- or di-C1-12alkylamino, C1-12alkyl- or arylamido, C1-12alkyl- or arylcarbonyl, C1-12alkyl- or arylcarboxy, C1-12alkyl- or arylcarbamoyl, C1-12alkyl, C2-12alkenyl, C2-12alkynyl, aryl, heteroaryl, C1-12alkoxy, aryloxy, azido, C1-12alkyl- or arylthio, C1-12alkyl- or arylsulfonyl, C1-12alkyl- or arylsilyl, C1-12alkyl- or arylphosphoryl, and phosphato; to form a compound of formula (II), wherein R, R', R1 and R2 are as defined for formula (I); said method comprising treating the compound of formula (I) with a palladium (0) catalyst and a (diphenylphosphino)nC1-6 alkane, wherein n is an integer of 1-6. The invention also provides methods of making penciclovir and famciclovir using this rearrangement reaction.

More Like This:

JP3059469	INDUSTRIAL APPLICABILITY: Antiviral quaternary ammonium salt and method for producing the same.
WO/1993/017020	THERAPEUTIC NUCLEOSIDES
WO/1997/049405	TOPICAL GEL COMPOSITION CONTAINING A COMBINATION OF A NSAID AND A XANTHINE DERIVATIVE

Inventors:

GEEN GRAHAM RICHARD (GB)
SHARE ANDREW COLIN (GB)

Application Number:

PCT/EP1999/002309

Publication Date:

February 17, 2000

Filing Date:

March 30, 1999

Export Citation:

Click for automatic bibliography generation Help

Assignee:

SMITHKLINE BEECHAM PLC (GB)
GEEN GRAHAM RICHARD (GB)
SHARE ANDREW COLIN (GB)

International Classes:

A61K31/52; A61K31/522; A61P31/12; C07D473/18; C07D473/32; C07D473/40; (IPC1-7): C07D473/40; C07D473/32; C07D473/18

Domestic Patent References:

WO1995028402A2

1995-10-26

Foreign References:

EP0352953A2	1990-01-31
EP0182024A2	1986-05-28
EP0141927A2	1985-05-22
US5684153A	1997-11-04

Other References:

B. M. CHOUDARY ET AL., NUCLEOSIDES & NUCLEOTIDES, vol. 15, no. 5, 1996, pages 981 - 94, XP002124799
N. J. LEONARD ET AL., JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, vol. 96, no. 18, September 1974 (1974-09-01), pages 5894 - 5903, XP002124800

Download PDF:

View/Download PDF PDF Help

Previous Patent: AZATRICYCLO[3.3.1.1] DECANE DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM

Next Patent: PYRROLO[1,2-a]PYRAZINE sPLA¿2? INHIBITOR