专利号:EP-2070941-A1 优先权日:2007-12-14 标 题 :Stereoselective synthesis of selective estrogen receptor down-regulators 权利人:BAYER SCHERING PHARMA AG; ASTRAZENECA AB 摘要:The present invention relates to stereoselective synthesis of 7-α-substituted estra-4-ene-3,17-diones. Such compounds are valuable intermediates in the synthesis of 7-α-substituted estra-1,3,5(10)-triene-3,17-diols. n Key step in this synthesis is reacting a 3-keto-4,6-estradiene with a Grignard reagent selected from the group consisting of a magnesium-halide alkyl halide having at least 3 carbon atoms, a magnesium-halide alkenyl halide having at least 3 carbon atoms, and a magnesium-halide alkynyl halide having at least 3 carbon atoms, in the presence of a catalyst system comprising CuI. n The obtained 7α-alkyl, alkenyl and alkynyl halides can be used for the synthesis of pharmaceutically actice 7-α-substituted estra-1,3,5(10)-triene-3,17-diols (antiestrogens).
专利号:US-4026911-A 优先权日:1976-02-23 标 题:Process for the preparation of ketoalkynoic acids and use of the process in an improved synthesis of 2-(substituted)-cyclo-pentane-1,3,4-triones 发明人:REVERMAN LAWRENCE FRANCIS 权利人:MILES LAB 摘要:Reaction of a 2-methyl-2-(alkenyl)-1,3-dioxolane with an α,ω-dihalogenoalkane to obtain a 2-methyl-2-(ω-chloroalkynyl)-dioxolane, conversion of the latter to a corresponding nitrile, and hydrolysis of the nitrile to form a ketoalkynoic acid is a novel process for preparing the acid. n Use of the process in the synthesis of 2-(substituted)-cyclopentane-1,3,4-triones improves that synthesis.
专利号:US-6159673-A 优先权日:1996-07-17 标 题:Oxonol compound, light-sensitive material and process for the synthesis of oxonol compound 发明人:NISHIGAKI JUNJI; DEGUCHI YASUAKI 权利人:FUJI PHOTO FILM CO LTD 摘要:An oxonol compound is represented by the following formula (I): in which Z is an atomic group that forms a cyclic amide ring; each of W1 and W2 independently is an atomic group that forms an acidic nucleus ring; and M is a cation. Other oxonol compounds, a light-sensitive material containing an oxonol compound and a process for the synthesis of an oxonol compound are also disclosed.
专利号:EP-1473330-B1 优先权日:1996-07-17 标题:Process for the synthesis of oxonol compound 发明人:NISHIGAKI JUNJI; DEGUCHI YASUAKI 权利人:FUJI PHOTO FILM CO LTD 摘要:An oxonol compound is represented by the following formula (I): in which each of Z, W<1> and W<2> independently is an atomic group that forms a heterocyclic ring; and M is a cation. A process for the synthesis of an oxonol compound is disclosed.
专利号:US-7321044-B2 优先权日:2001-10-12 标题 :Synthesis of oxygen-substituted benzocycloheptenes as valuable intermediate products for the production of tissue-selective estrogens 发明人:PLATZEK JOHANNES; BECKMANN WOLFGANG; GEISLER JENS; KIRSTEIN HOLGER; NIEDBALLA ULRICH; OTTOW ECKHARD; RADAU SIGMAR; SCHULZ CLAUDIA; WESSA THOMAS 权利人:SCHERING AG 摘要:The invention relates to intermediate products and a new process for the production of benzocycloheptene C. n n n n n n n n n n The process for the production of its new intermediate products according to the invention starts from economical starting materials, provides the intermediate stages in high yields and high purity, without chromatographic purification steps, and allows production on an industrial scale.
专利号:US-2009264648-A1 优先权日:2008-01-14 标题:Synthesis of pyrazoles 发明人:CHEW WARREN; WANG ZHENG; CHEAL GLORIA; BERTRAND MARTIAL; POTOSKI JOHN; MIRMEHRABI MAHMOUD; NENCINI ARIANNA; ZANALETTI RICCARDO 权利人:WYETH CORP; SIENA BIOTECH SPA 摘要:The present invention provides compounds and compositions, methods of making them, and methods of using them to modulate α7 nicotinic acetylcholine receptors and/or to treat any of a variety of disorders, diseases, and conditions. Provided compounds can affect, among other things, neurological, psychiatric and/or inflammatory system.
摘要:Li, L.; Biscoe, M. R., Science of Synthesis: Cross Coupling and Heck-Type Reactions, (2012) 1, 797. 摘要:Shu, X.-Z.; Pang, X., Science of Synthesis: Special Topics, (2022) 1, 404.