Process for the preparation of purine derivatives

Organic compounds -- part of the class 532-570 series – Organic compounds – Chalcogen bonded directly to ring carbon of the purine ring...

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544277, C07D47318, C07D47332

Patent

active

056841531

ABSTRACT:
The present invention provides a process for the synthesis of penciclovir and famciclovir by 9-substituting the compound 2-amino-6-chloropurine (ACP) with 2-acetoxymethyl-4-(leaving group)-but-1-yl acetate, followed by displacement of the 6-chloro moiety with a hydroxy moiety (i.e. to form a guanine derivative) or with hydrogen (to form the 2-aminopurine derivative), respectively.

REFERENCES:
patent: 5075445 (1991-12-01), Jarvest et al.
patent: 5246937 (1993-09-01), Harnden et al.
Geen et al., Tetrahedron, 46:19, 6903-6914, (1990).
Chu et al., J. Heterocyclic Chem., 23, 289 (1986).
Robins et al., Can. J. Chem., 60 (1982).
Kjellberg et al., Nucleosides & Nucleotides, 8:2, 225-256 (1989).

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