专利号:US-7173021-B2 优先权日:2004-09-02 标题:Synthesis of temozolomide esters as potent anticancer pro-drugs for topical and transdermal applications in treatments of cancers 发明人:WANG YONGFENG; CONWAY BARBARA R; SUPPASANSATORN PANASSAYA 权利人:TIANJIN NORTH PHARM SCI TECH C 摘要:This invention relates to the use of temozolomide esters (4-dihydro-3-methyl-4-oxoimidazo[5,1-d]-1,2,3,5-tetrazine-8-carboxylate esters) Formula 1 as potent anticancer pro-drugs for treatment of cancers by topical and transdermal applications, and to a novel process for synthesis of temozolomide esters by a direct esterification of temozolomide acid (3,4-dihydro-3-methyl-4-oxoimidazo[5,1-d]-1,2,3,5-tetrazine-8-carboxylic acid) with a halogeno-aliphatic compound in presence of a base, or with an alcohol in presence of a dehydrate agent
专利号:US-4412958-A 优先权日:1981-10-16 标 题:Stereospecific synthesis of 5-phenyl-2S-pentanol 发明人:CUE JR BERKELEY W; MOORE BERNARD S 权利人:PFIZER 摘要:5-Phenyl-2S-pentanol is synthesized stereospecifically from S ethyl lactate. The method provides easily purified 5-phenyl-2S-pentanol useful in the synthesis of central nervous system active (CNS) agents such as levonantradol.
专利号:US-2007293456-A9 优先权日:2004-12-30 标题:Method for the synthesis of 3-substituted indolizine and benzoindolizine compounds 发明人:HAYFORD ANTHONY; KALOKO JOSEPH 权利人:HAYFORD ANTHONY; KALOKO JOSEPH 摘要:A method of making a compound of Formula I: n n ncomprises reacting a compound of Formula II n n nwith a compound such as R 1 OH or R 1 SH, to produce said compound of Formula I. Compounds of Formula I are useful, among other things, as dyes, spectral sensitizers, glycosidase inhibitors, and as antibacterial, antiviral, and anti-inflammatory agents.
专利号:US-2004053999-A1 优先权日:1997-09-17 标题 :Novel compounds and methods for synthesis and therapy 发明人:BISCHOFBERGER NORBERT W; DAHL TERRENCE C; HITCHCOCK MICHAEL J M; KIM CHOUNG U; LEW WILLARD; LIU HONGTAO; MILLS ROGER G; WILLIAMS MATTHEW A 摘要:Novel compounds are described. The compounds generally comprise an acidic group, a basic group, a substituted amino or N-acyl and a group having an optionally hydroxylated alkane moiety. Pharmaceutical compositions comprising the inhibitors of the invention are also described. Methods of inhibiting neuraminidase in samples suspected of containing neuraminidase are also described. Antigenic materials, polymers, antibodies, conjugates of the compounds of the invention with labels, and assay methods for detecting neuraminidase activity are also described.
专利号:US-2022411449-A1 优先权日:2019-11-13 标 题 :Method for Preparing Heteroleptic Triarylbismuthanes and Compounds Produced by the Same 发明人:HYVL JAKUB; LEHRER AXEL 权利人:UNIV HAWAII 摘要:A method for controlling dismutation in the synthesis of a heteroleptic triarylbismuthane is provided as are compounds produced by such a method and use of the same to inhibit the replication of microorganisms.
专利号:US-6225341-B1 优先权日:1995-02-27 标 题:Compounds and methods for synthesis and therapy 发明人:BISCHOFBERGER NORBERT W; KIM CHOUNG U; LEW WILLARD; LIU HONGTAO; WILLIAMS MATTHEW A 权利人:GILEAD SCIENCES INC 摘要:Novel compounds are described. The compounds generally comprise an acidic group, a basic group, a substituted amino or N-acyl and a group having an optionally hydroxylated alkane moiety. Pharmaceutical compositions comprising the inhibitors of the invention are also described. Methods of inhibiting neuraminidase in samples suspected of containing neuraminidase are also described. Antigenic materials, polymers, antibodies, conjugates of the compounds of the invention with labels, and assay methods for detecting neuraminidase activity are also described.
[参考文献]: H G Abbas, Et Al. Synthesis Of [参考文献]: Shintaro Tobiishi, Et Al. Methoxy- And Fluorine-Substituted Analogs Of O-1302: Synthesis And In Vitro Binding Affinity For The Cb1 Cannabinoid Receptor. Chem Pharm Bull (Tokyo). 2007 Aug;55(8):1213-7.
合成参考文献
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