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Generated: August 21, 2017

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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 2-amino-6-chloropurine (ACP) with an appropriate side chain precursor, followed by conversion of the 6-chloro moiety to a hydroxy moiety (i.e. to form a guanine) or hydrogen (to form a 2-aminopurine), respectively.
Inventor(s): Geen; Graham Richard (Dunmow, GB), Jarvest; Richard Lewis (Ware, GB)
Assignee: Novartis International Pharmaceutical Ltd. (Hamilton, BM)
Filing Date:Dec 11, 2000
Application Number:09/734,051
Claims:1. A process for the preparation of i) penciclovir or ii) famciclovir which process comprises:

i) hydrolysing 9-(4-acetoxy-3-acetoxymethylbut-1-yl)-2-amino-6-chloropurine to give penciclovir; or

ii) reducing 9-(4-acetoxy-3-acetoxymethylbut-1-yl)-2-amino-6-chloropurine to give famciclovir.

2. A compound known as 9-(4-acetoxy-3-acetoxymethylbutyl)-2-amino-6-chloropurine.
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US Army
Fish and Richardson
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Farmers Insurance

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