专利号:US-5349099-A 优先权日:1993-12-13 标题:Process for preparing intermediates for the synthesis of antifungal agents 发明人:KUO SHEN-CHUN; HOU DONALD; ZHAN ZHENG-YUN 权利人:SCHERING CORP 摘要:Disclosed is a process for preparing allylic halides of the formula I ##STR1## wherein X is Cl, Br or I, for use as intermediates in the synthesis of substituted tetrahydrofuran azole anti-fungal agents.
专利号:US-7342003-B2 优先权日:2001-10-25 标 题 :Synthesis of 2-aralkyloxyadenosines, 2-alkoxyadenosines, and their analogs 发明人:MOORMAN ALLAN R; SCANNELL MICHAEL; BALASUBRAMANIAN THIAGARAJAN; OUTCALT RUSSELL; LEUNG EDWARD 权利人:KING PHARMACEUTICALS RES & DEV 摘要:Provided is a method for the synthesis of an aralkyloxyadenosine or an alkoxyadenosine. The method includes protecting the hydroxyl sugar groups with a protecting group to produce a protected halogenated adenosine. The protected halogenated adenosine is alkoxylated, and the hydroxyl sugar groups of the protected halogenated adenosine are deprotected to provide the aralkyloxyadenosine or alkoxyadenosine.
专利号:US-2015376219-A1 优先权日:2014-06-30 标题 :Selective Preparations of Purine Nucleosides and Nucleotides: Reagents and Methods 发明人:ZHONG MINGHONG 权利人:ZHONG MINGHONG 摘要:A process of regiospecific synthesis of N-9 purine nucleoside analogs in either solution or solid phase synthesis is described. The introduction of the sugar moiety or its analogue on to a 6-heteroarylium purine or its mesomeric betaine so that formation of only the N-9 position regioisomers of the purine nucleoside analogs (either D or L enantiomers) is obtained. This regiospecific introduction of the sugar moiety allows the synthesis of purine nucleoside analogs in high yields without formation of the N-7-positional regioisomers, while the 6-heteroaryliums are leaving groups facilitated for nucleophilic displacement. Solid supported 6-heterarylium purine bases can be used for purine based library synthesis and synthesis of nucleotide monophosphates and polyphosphates. Processes for providing novel 6-heteroarylium purines and their corresponding mesomeric betaines for the regiospecific synthesis of N-9 purine nucleoside analogs and nucleotides are described.
专利号:US-6884880-B2 优先权日:2002-08-21 标 题:Process for the preparation of 9-β-anomeric nucleoside analogs 发明人:GUPTA PRANAB K; MUNK STEPHEN A 权利人:ASH STEVENS INC 摘要:A process for substantially enhancing the regio and stereoselective synthesis of 9-β-anomeric nucleoside analogs is described. The introduction of the sugar moiety onto a 6-substituted purine base was preformed so that only the 9-β-D- or L-purine nucleoside analogs were obtained. This regio and stereoselective introduction of the sugar moiety allows the synthesis of nucleoside analogs and in particular 2′-deoxy, 3′-deoxy, 2′-deoxy-2′-β-fluoro and 2′,3′-dideoxy-2′-β-fluoro purine nucleoside analogs in high yield without virtually any formation of the 7-positional isomers. The compounds are drugs or intermediates to drugs.
专利号:US-2006199958-A1 优先权日:2003-04-14 标 题 :Process and intermediates for the preparation of pyrrolidine carboxylic acids 发明人:CVETOVICH RAYMOND; CHUNG JOHN Y; AMATO JOSEPH S; DIMICHELE LISA 权利人:CVETOVICH RAYMOND; CHUNG JOHN Y; AMATO JOSEPH S; DIMICHELE LISA 摘要:A novel process is provided for the preparation of pyrrolidine carboxylic acids, and the useful intermediates obtained therein. These compounds are intermediates for the synthesis of melanocortin-4 receptor (MC-4R), which are useful for the treatment of disorders such as obesity, diabetes, sexual dysfunction, male sexual dysfunction, and female sexual dysfunction.
专利号:US-5132437-A 优先权日:1991-02-12 标题:Synthesis of 1-aminoanthraquinone 发明人:ASLAM MOHAMMAD; AGUILAR DANIEL A 权利人:HOECHST CELANESE CORP 摘要:1-Aminoanthraquinone (1-AAQ) is synthesized by the reaction of 2-chlorobenzyl chloride and xylene in the presence of a solid acid catalyst to yield 2-chloro dimethyldiphenylmethane, subsequent oxidation of the methyl groups, ring closure to form a 1-chloroanthraquinone carboxylic acid, replacement of the 1-chloro group with ammonia, and decarboxylation.