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Title:
METHODS OF SYNTHESIS FOR 9-SUBSTITUTED HYPOXANTHINE DERIVATIVES
Document Type and Number:
WIPO Patent Application WO2002000659
Kind Code:
A3
Abstract:
An improved method of systhesis of a 9-substituted hypoxanthine derivative comprises the steps of: (1) reacting aminocyanacetamide with triethyl orthoformate to form an imidoester derivative of aminocyanacetamide; (2) forming a compound having a reactive amino group on a hydrocarbyl moiety, the hydrocarbyl moiety being linked through an amide group to a physiologically active moiety or an esterified derivative of a physiologically active moiety including therein an esterified benzoyl group; (3) reacting the imidoester with the compound having the reactive amino group on the hydrocarbyl moiety to form a derivative of 5-aminoimidazole-4-carboxamide substituted at the 1-position with a hydrocarbyl moiety linked through an amide group to a physiologically active moiety including therein an optionally esterified benzoyl group; (4) forming the six-membered heterocyclic ring of the purine moiety of the hypoxanthine by reacting the derivative of 5-aminoimidazole-4-carboxamide formed in step (3) with triethyl orthoformate to form a 9-substituted hypoxanthine compound substituted at the 9-position with a hydrocarbyl moiety linked through an amide group to a physiologically active moiety including therein an optionally esterified benzoyl group; and (5) hydrolyzing the ester of the optionally esterified group if present.

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Inventors:
GLASKY ALVIN (US)
BOLLINGER HEINRICH (CH)
MUELLER HANS RUDOLF (CH)
Application Number:
PCT/US2001/040908
Publication Date:
March 21, 2002
Filing Date:
June 08, 2001
Export Citation:
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Assignee:
NEOTHERAPEUTICS INC (US)
GLASKY ALVIN (US)
BOLLINGER HEINRICH (CH)
MUELLER HANS RUDOLF (CH)
International Classes:
A61P25/28; C07D233/88; C07D233/90; C07D473/30; (IPC1-7): C07D233/88; C07D473/30; A61K31/522; A61P25/28
Foreign References:
US5091432A1992-02-25
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