专利号:US-7737284-B2 优先权日:2001-01-18 标题 :Synthesis of temozolomide and analogs 发明人:KUO SHEN-CHUN; MAS JANET L; HOU DONALD CHEN-TUNG 权利人:SCHERING PLOUGH CORP 摘要:This invention relates to a novel process for the synthesis of Temozolomide, an antitumor compound, and analogs, and to intermediates useful in this novel process.
专利号:US-6849735-B1 优先权日:2000-06-23 标 题:Methods of synthesis for 9-substituted hypoxanthine derivatives 发明人:GLASKY ALVIN J; BOLLINGER HEINRICH; MUELLER HANS RUDOLF 权利人:MERCK EPROVA AG 摘要:An improved method of synthesis 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 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 benzoyl group if present.
专利号:US-2002156277-A1 优先权日:2001-04-20 标题 :Synthesis and methods of use of purine analogues and derivatives 发明人:FICK DAVID B; FOREMAN MARK M; GLASKY ALVIN J 摘要:A purine derivative or analogue comprises a 9-atom bicyclic moiety, moiety A, linked through a linker L to a moiety B, where B is a carboxylic acid, a carboxylic acid ester, or a moiety of the structure N(Y 1 )—D, where Y 1 can be one of a variety of substituents, including hydrogen or alkyl, and D is a moiety that enhances the pharmacological effects, promotes absorption or blood-brain barrier penetration of the derivative or analogue. The moiety A has a six-membered ring fused to a five-membered ring. The moiety A can have one, two, or three nitrogen atoms in the five membered ring and has two nitrogen atoms in the six-membered ring. The moiety A can be a purine moiety. The moiety B can be one of a variety of moieties, including moieties having nootropic activity or other biological or physiological activity.
专利号:US-2005131227-A1 优先权日:2001-01-18 标 题:Synthesis of temozolomide and analogs
专利号:US-2006229456-A1 优先权日:2001-01-18 标 题:Synthesis of Temozolomide and analogs
专利号:WO-02057269-A1 优先权日:2001-01-18 标题:Synthesis of temozolomide and analogs