专利号:WO-0027627-A1 优先权日:1998-11-12 标题 :Aryloxime linkers in the solid-phase synthesis of 3-aminobenzisoxazoles 发明人:WILEY MICHAEL ROBERT; LEPORE SALVATORE DONATO 权利人:LILLY CO ELI; WILEY MICHAEL ROBERT; LEPORE SALVATORE DONATO 摘要:In its first aspect, the invention is directed to a solid support mediated method for the synthesis of diverse polycyclic heterocycles according to general formula (V). A second aspect of the invention is directed to a solid support bound intermediate compound that optionally can be derivatized before a cyclization and displacement procedure provides a product. The intermediate is preferably stable to a wide range of chemical conditions thus allowing, if desired, for the chemical derivatization of the intermediate. A third aspect of the invention is directed to a library of polycyclic heterocycle compounds where said library contains a plurality of diverse library compounds of general formula (V). A fourth aspect of the invention is directed to a method for the synthesis of a library of diverse polycyclic heterocycles by the general method described. A fifth aspect of the invention is directed to an assay kit for the identification of lead compounds of the library described therein.
专利号:US-7276637-B2 优先权日:2002-08-02 标题:Synthesis of cyclohexanone derivatives 发明人:BRANDS KAREL MARIE JOSEPH; DAVIES ANTONY JOHN; OAKLEY PAUL JOSEPH; SCOTT JEREMY PETER; SHAW DUNCAN EDWARD; TEALL MARTIN RICHARD 权利人:MERCK & CO INC 摘要:A novel process for preparing cyclohexanone derivatives of formula (I) n nis described. The products are useful as gamma secretase inhibitors, or as intermediates in the synthesis of other gamma secretase inhibitors.
专利号:US-9926291-B2 优先权日:2007-03-27 标 题 :Synthesis of thiohydantoins 发明人:OUERFELLI OUATHEK; DILHAS ANNA; YANG GUANGBIN; ZHAO HONG 权利人:SLOAN KETTERING INST CANCER RES 摘要:A novel synthesis of the anti-androgen, A52, which has been found to be useful in the treatment of prostate cancer, is provided. A52 as well as structurally related analogs may be prepared via the inventive route. This new synthetic scheme may be used to prepare kilogram scale quantities of pure A52.
专利号:US-9085538-B2 优先权日:2010-07-26 标题:Process for the preparation of key intermediates for the synthesis of statins or pharmaceutically acceptable salts thereof 发明人:CASAR ZDENKO; STERK DAMJAN; JUKIC MARKO 权利人:CASAR ZDENKO; STERK DAMJAN; JUKIC MARKO; LEK PHARMACEUTICALS 摘要:The invention relates to commercially viable process for the synthesis of key intermediates for the preparation of statins, in particular Rosuvastatin and Pitavastatin or respective pharmaceutically acceptable salts thereof. A new simple and short synthetic route for key intermediates is presented which benefits from the use of cheap and readily available starting materials, by which the conventionally most frequently used DIBAL-H as reducing agent can be avoided.
专利号:US-9035013-B2 优先权日:2010-08-04 标 题 :Sulphur-containing triazine monomer that can be used for the synthesis of a polymer membrane for a fuel cell 发明人:FEDURCO MILAN 权利人:FEDURCO MILAN; MICHELIN & CIE; MICHELIN RECH TECH 摘要:A sulphur-containing triazine monomer is provided that can be used in the synthesis of a polymer membrane for a PEM-type fuel cell. The sulphur-containing triazine monomer has a structure corresponding to a formula (I): n nin which:n Tz represents a 1,3,5-triazine nucleus; X 1 and X 2 , which are identical or different, represent S, SO, or SO 2 ; Ar 1 , Ar 2 , Ar 4 and Ar 5 , which are identical or different, represent a substituted or unsubstituted phenylene group; Ar 3 represents a substituted or unsubstituted phenyl group; and Z 1 and Z 2 , which are identical or different, are selected from a group that includes halogens, hydroxyl, alkoxyl, thiol, carboxyl, carboxylates, amine, sulphonamide, acyl chlorides, sulphonyl chlorides, sulphonyl fluorides, isocyanates, and combinations thereof.
专利号:WO-2009148195-A1 优先权日:2008-06-02 标题:5-(4-hydroxybenzyl)thiazolidine-2,4-dione as intermediate for synthesis of thiazolidinedione based compounds and process for preparing the same 发明人:PARK JIN OH; KIM YONG GIL; SON HAN IL; LEE YUN JEONG; KIM EUN MI 权利人:DAEBONG LS LTD; PARK JIN OH; KIM YONG GIL; SON HAN IL; LEE YUN JEONG; KIM EUN MI 摘要:The present invention relates to 5-(4-hydroxybenzyl)thiazolidine-2,4-dione represented by the following Chemical Formula [1], which is useful as an intermediate for synthesis of thiazolidinedione based compounds, a method for preparing the compound, and a method for preparing pioglitazone or pioglitazone hydrochloride, which is a thiazolidinedione based drug and useful in treating and preventing diabetes, using the 5-(4-hydroxybenzyl)thiazolidine-2,4-dione represented by Chemical Formula [1] as an intermediate:
[参考文献]: Eric J Schelter, Et Al. Actinide-Mediated Coupling Of 4-Fluorobenzonitrile: Synthesis Of An Eight-Membered Thorium(Iv) Tetraazametallacycle. Chem Commun (Camb). 2007 Mar 14:(10):1029-31.
合成参考文献
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