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Generated: January 18, 2018

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Title: Process for the preparation of purine derivatives
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.
Inventor(s): Geen; Graham Richard (Stansted Mountfitchet, GB2), Jarvest; Richard Lewis (Surbiton, GB2)
Assignee: Beecham Group plc (Brentford, GB)
Filing Date:Jun 10, 1994
Application Number:08/258,167
Claims:1. 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:


ii) reducing to give famciclovir.

2. A process according to claim 1 wherein the leaving group is halo.

3. A process according to claim 2 wherein the halogen is chlorine.

4. A process according to claim 2 wherein the halogen is bromine.

5. A process according to claim 2 wherein the halogen is iodine.
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Serving leading biopharmaceutical companies globally:

US Department of Justice
Queensland Health
Farmers Insurance
Boehringer Ingelheim
Federal Trade Commission
Cantor Fitzgerald

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