Patent · US Expired

Process for the preparation of 2'-O-alkyl purine phosphoramidites

US5646265A · kind A · utility

456Cited by
3References
15Claims
0Family size

Assignee

Inventor

Key dates

Filing dateMar 23, 1995
Grant dateJul 8, 1997
Priority date—
Expiry dateMar 23, 2015

Classification

  • Technology area (CPC C)Chemistry; Metallurgy
  • CPC primaryC12N2310/3533
  • WIPO fieldPharmaceuticals
  • WIPO sectorChemistry

Abstract

2'-O-alkylated guanosine, uridine, cytidine, and 2,6-diaminopurine 3'-O-phosphoramidites are prepared by alkylating nucleoside precursors, adding suitable blocking groups and phosphitylating. Alkylation is effected on 2,6-diamino-9-(.beta.-D-ribofuranosyl)purine followed by deamination to prepare guanosine 2'-O-alkylated 3'-O-phosphormidites. Alkylation is effected on a dialkyl stannylene derivative of uridine to prepare uridine 2'-O-alkylated 3'-O-phosphormidites. Alkylation is effected directly on cytidine to prepare cytidine 2'-O-alkylated 3'-O-phosphormidites. Alkylation is effected directly on 2,6-diaminopurine to prepare 2,6-diaminopurine 2'-O-alkylated 3'-O-phosphormidites.

Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.