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US 5,684,153 AGranted
Process for the preparation of purine derivatives
AssigneeBeecham Group Limited
InventorsGraham Richard Geen, Richard Lewis Jarvest
Life of this patent
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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.
Claims5
A process for the preparation of i) penciclovir or ii) famciclovir which process comprises the reaction of 2-amino-6-chloropurine with 2-acetoxymethyl-4-(leaving group)-but-1-yl acetate;
- to give 9-(4-acetoxy-3-acetoxymethylbut-1-yl)-2-amino-6-chloropurine;
- and thereafter:
- i) hydrolysing to give penciclovir:
- or
- ii) reducing to give famciclovir.
2 more elements
Dependencies are inferred from the claim text.