Methods for the synthesis of substituted purines
US6949644B2 · kind B2 · utility
Assignees
Inventors
Key dates
| Filing date | Oct 12, 2002 |
| Grant date | Sep 27, 2005 |
| Priority date | — |
| Expiry date | Dec 3, 2022 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07D473/16
- WIPO fieldOrganic fine chemistry
- WIPO sectorChemistry
Abstract
The invention provides general methods for preparing 2,9-, 2,6,9-, O6-aryl- and O6-alkyl-substituted purines in a combinatorial and traceless fashion. The methods involve, in some embodiments, Mitsunobu alkylation of 2-fluoro-6-phenylsulfenylpurine at N9 with alcohols in solution, followed by C2-capture of the purine core with a resin-bound amine and subsequent oxidation and displacement of the C6 sulfonyl group with amines and anilines. In one aspect, the present invention provides a method of preparing a 2,6,9-substituded purine compounds of Formula I: the method comprising:
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.