专利号:US-8759555-B2 优先权日:2004-03-18 标 题:Stereoselective synthesis of vitamin D analogues 发明人:SABROE THOMAS PETER; CALVERLEY MARTIN JOHN 权利人:SABROE THOMAS PETER; CALVERLEY MARTIN JOHN; LEO PHARMA AS 摘要:The present invention relates to intermediates useful for the synthesis of calcipotriol or calcipotriol monohydrate, to methods of producing said intermediates, and to methods of stereoselectively reducing said intermediates.
专利号:US-8410267-B2 优先权日:2008-11-27 标 题 :Regioselective reduction of fused pyrrolocarbazoles-5,7-diones 发明人:PRAT-LACONDEMINE LAURENCE 权利人:PRAT-LACONDEMINE LAURENCE; TEVA SANTE 摘要:The present invention relates to a method for regioselectively reducing the maleimide compounds of formula (I). The invention also relates to C 7 hydroxy lactam regioisomers of formula (II) obtainable by this method and their use for the preparation of lactams of formula (III) which are particularly useful as intermediate for the synthesis of fused pyrrolocarbazoles.
专利号:US-4209464-A 优先权日:1977-06-10 标题:Novel synthesis of 3-amino-2-methylbenzotrifluoride from N-(2-X-5-trifluoromethylphenyl)-S,S-dimethylsulfimide 发明人:STEINMAN MARTIN; WONG YEE S 权利人:SCHERING CORP 摘要:This invention relates to a novel process for preparing 3-amino-2-methylbenzotrifluoride, and to certain novel intermediates produced by the process. 3-Amino-2-methylbenzotrifluoride is a key intermediate useful in the preparation of valuable therapeutic agents such as, for example, 2-(2-methyl-3-trifluoromethyl)anilino nicotinic acid.
专利号:US-2007232813-A1 优先权日:2006-03-28 标 题:Substituted Cyclohexadienals - Syntheses and Applications 发明人:WATANABE CORAN M H; BENCH BENNIE JOHN 权利人:WATANABE CORAN M H; BENCH BENNIE JOHN 摘要:The present invention is generally directed to the use of L-proline and certain derivatives thereof to catalyze the asymmetric self-condensation of α,β-unsaturated aldehydes to form homodimer and heterodimer cyclohexadienals. Reaction conditions are mild and yet amenable to a variety of different substrates yielding molecules with complex scaffolds from simple precursors. This approach allows for diversification and synthesis of this structural class of compounds in sufficient quantity, purity and enantioselectivity for, e.g., biological investigations and use as fluorescent probes, anti-cancer agents, anti-bacterial agents, and/or anti-fungal agents. The present invention is also generally directed to the cyclohexadienals produced.
专利号:US-7320993-B1 优先权日:1997-12-17 标题 :Aryl-substituted pyridylalkane, alkene, and alkine carboxamides useful as cytostatic useful as cytostatic and immuosuppressive agents 发明人:BIEDERMANN ELFI; HASMANN MAX; LOESER ROLAND; RATTEL BENNO; REITER FRIEDEMANN; SCHEIN BARBARA; SEIBEL KLAUS; VOGT KLAUS; WOSIKOWSKI KATJA; SCHEMAINDA ISABEL 权利人:ASTELLAS DEUTSCHLAND GMBH 摘要:The invention relates to new pyridylalkane, alkene, and alkine acid amides substituted with an aryl and/or heteroaryl residue according to the general formula (I), with a saturated or one or several-fold unsaturated hydrocarbon residue in the carboxylic acid group, methods for the synthesis of these compounds, medicaments containing these and their production as well as their therapeutic use, especially as cytostatic agents and immunosuppressive agents, for example in the treatment or prevention of various types of tumors and control of immune reactions such as autoimmune diseases.
专利号:CA-2555260-C 优先权日:2004-03-18 标 题 :Stereoselective synthesis of vitamin d analogues
[参考文献]: K U Ingold, Et Al. Isomerization Of Triphenylmethoxyl And 1,1-Diphenylethoxyl Radicals. Revised Assignment Of The Electron-Spin Resonance Spectra Of Purported Intermediates Formed During The Ceric Ammonium Nitrate Mediated Photooxidation Of Aryl Carbinols. J Org Chem. 2006 Dec 22;71(26):9906-8.
合成参考文献
摘要:Kostikov, R. R.; Khlebnikov, A. F.; Sokolov, V. V., Science of Synthesis, (2010) 47, 803. 摘要:García-Garrido, S. E.; Presa Soto, A.; García-Álvarez, J., Science of Synthesis: Knowledge Updates, (2025) 2. 摘要:García-Garrido, S. E.; Presa Soto, A.; García-Álvarez, J., Science of Synthesis: Knowledge Updates, (2025) 2.