专利号:US-5760249-A 优先权日:1995-08-29 标题 :Synthesis of hydroxysulfone and related compounds 发明人:MATHRE DAVID J; SOHAR PAUL; MOODY DAVID; BLACKER ANDREW J 权利人:MERCK & CO INC; ZENECA LTD 摘要:This invention is concerned with an improved process for the synthesis of hydroxysulfone, which is a key intermediate in the synthesis of carbonic anhydrase inhibitors, especially dorzolamide. Carbonic anhydrase inhibitors are known to be effective in treating elevated intraocular pressure or glaucoma.
专利号:EP-0853625-B1 优先权日:1995-08-29 标 题:Synthesis of hydroxysulfone and related compounds 发明人:MATHRE DAVID J; SOHAR PAUL; MOODY DAVID; BLACKER ANDREW J 权利人:MERCK & CO INC; SYNGENTA LTD 摘要:This invention is concerned with an improved process for the synthesis of hydroxysulfone, which is a key intermediate in the synthesis of carbonic anhydrase inhibitors, especially dorzolamide. Carbonic anhydrase inhibitors are known to be effective in treating elevated intraocular pressure or glaucoma.
专利号:US-2005165238-A1 优先权日:2001-12-19 标题 :Oxidation process for the preparation of intermediates useful in the synthesis of diarylpyridines 发明人:CANNATA VINCENZO; SORIATO GIORGIO; VERZINI MASSIMO 摘要:An oxidation process for the preparation of intermediates useful in the synthesis of diarylpiridines is described. The oxidation of the thioether of formula III to give the sulfone of formula II is is carried out with a mixture of peracetic acid and hydrogen peroxide as oxidant, in the presence of methanesulphonic acid and in the absence of a catalylst.
专利号:US-9024030-B2 优先权日:2012-01-13 标题 :Process for the synthesis of etoricoxib 发明人:MAO ZHENMIN; LAN TIAN; LIU LANFANG; YAN LONG; BECKER STEFAN 权利人:TIEFENBACHER ALFRED E GMBH & CO KG; SHANGHAI GOLDEN PHARMATECH CO LTD; SHANGHAI GOLDEN PHARMATECH CO LTD 摘要:The present invention relates to a process for the synthesis of the anti-inflammatory agent 5-chloro-3-(4-methanesulfonylphenyl)-6′-methyl-[2,3′]bipyridine, referred to as compound of formula (1) or etoricoxib, which is a pharmaceutically active ingredient inhibiting cyclooxygenase-2. In particular, the application concerns a novel process of making the compound of formula (1) by oxidizing a compound of formula (4).
专利号:US-8664402-B2 优先权日:2011-03-09 标题:Process for preparing 1-(6-methylpyridin-3-yl)-2-[4-(methylsulfonyl)phenyl]ethanone, an intermediate of etoricoxib 发明人:CASTELLIN ANDREA; STABILE PAOLO; FONTANA FRANCESCO; DE LUCCHI OTTORINO; CAPORALE ANDREA; TARTAGGIA STEFANO 权利人:CASTELLIN ANDREA; STABILE PAOLO; FONTANA FRANCESCO; DE LUCCHI OTTORINO; CAPORALE ANDREA; TARTAGGIA STEFANO; ITALIANA SINT SPA 摘要:A process for preparing 1-(6-methylpyridin-3-yl)-2-[4-(methyl sulfonyl)phenyl]ethanone, an intermediate of the synthesis of Etoricoxib. The synthesis of the intermediates useful for such preparation is also described.
专利号:US-5157129-A 优先权日:1990-04-18 标题:Enantiospecific synthesis of s-(+)-5,6-dihydro-4-(r-amino)-4h-thieno(2,3-b)thiopyran-2-sulfonamide-7,7-dioxide 发明人:BLACKLOCK THOMAS J; JONES TODD K; GRABOWSKI EDWARD J J; MATHRE DAVID J; MOHAN JULIE J; SOHAR PAUL; ROBERTS F EDWARD; XAVIER LYNDON C 权利人:MERCK & CO INC 摘要:5,6-Dihydro-4-(R-amino)-4H-thieno[2,3-b]-thiopyran-2-sulfonamide-7,7-dioxide is a potent carbonic anhydrase inhibitor useful in the treatment of ocular hypertension and glaucoma. The S-(+)-enantiomer of that compound, the more active enantiomer, is prepared by a process involving an intermediate step of an enantioselective reduction of a carbonyl group employing an oxazaborolidine chiral catalyst.
参考标题:Access To Pyridines Via Cascade Nucleophilic Addition Reaction Of 1,2,3-Triazines With Activated Ketones Or Acetonitriles 作者:Yuan Zhang,Han Luo,Qixing Lu,Qiaoyu An,You Li,Shanshan Li,Zongyuan Tang,Baosheng Li |发布日期:2021.1 摘要:Cascade Nucleophilic Addition Reactions Of 1,2,3-Triazines With Activated Acetonitriles Or Ketones, Which Were Used To Construct Highly Substituted Pyridines That Are Not Easily Accessed By Conventional Methods. The Strategy Addressed Some Structural Diversity Issues Currently Facing Medicinal Chemistry, And The Resulting Pyridines Could Be Used As Convenient Precursors For The Synthesis Of Related Pharmaceuticals
合成参考文献
摘要:Kleemann, A.; Engel, J.; Kutscher, B.; Reichert, D., Pharmaceutical Substances[Online], Thieme: Stuttgart, (2004). 摘要:Spitzner, D., Science of Synthesis, (2005) 15, 201.