专利号:US-3901922-A 优先权日:1972-04-25 标题 :Synthesis of zearalanone and related compounds and intermediates useful in their synthesis 发明人:URRY WILBERT HERBERT; MULLENBACH GUY TOWNS 权利人:COMMERCIAL SOLVENTS CORP 摘要:WHEREIN X is an integer having a value from 2 to 6 inclusive and Y is an integer having a value from 2 to 8 inclusive. It also provides for new methods of making compounds useful in the synthesis of zearalanone and related compounds. The new compounds useful as intermediates are 2,7-octadienoic acid; methyl 2,7-octadienoate; sodium ethyl 6-(4-pentenyl)- Beta -dihydroesorcylate; ethyl 6-(4-pentenyl)- Beta dihydroresorcylate; sodium methyl 6-(4-pentenyl)- Beta dihydroresorcylate; methyl 6-(4-pentenyl)- Beta dihydroresorcylate; methyl 3-bromo-6-(4-pentenyl)- Beta dihydroresorcylate; methyl 6-(4-pentenyl)- Beta -resorcylate; ethyl 6-(4-pentenyl)- Beta -resorcylate; ethyl 6-(4-pentenyl)Beta -resorcylate dibenzyl ether; tetrahydropyran-2-yl 4-penten2-yl ether; ethyl 6-(6-oxo-10-tetrahydropyran-2-xyloxyundecyl)Beta -resorcylate dibenzyl ether; and 6-(10-hydroxy-6oxounderyl)- Beta -resorcylic acid dibenzyl ether. Methods for preparing these intermediates are also disclosed. This invention provides a new synthesis for zearalanone and for related compounds having more or fewer carbon atoms in the nonaromatic ring than does zearalanone, which related compounds and zearalanone are represented by the formula
专利号:US-3810918-A 优先权日:1972-04-25 标题:Synthesis of zearalanone 发明人:URRY W; MULLENBACH G 权利人:COMMERCIAL SOLVENT CORP 摘要:4,5-(-COO-CH(-CH3)-(CH2)X-CO-(CH2)Y-)RESORCINOL THIS INVENTION PROVIDES A NEW SYNTHESIS FOR ZEARALANONE AND FOR RELATED COMPOUNDS HAVING MORE OR FEWER CARBON ATOMS IN THE NON-AROMATIC RING THAN DOES ZEARLANONE, WHICH RELATED COMPOUNDS AND ZEARALANONE ARE REPRESENTED BY THE FORMULA WHEREIN X IS AN INTEGER HAVING A VALUE FROM 2 TO 6 INCLUSIVE AND Y IS AN INTEGER HAVING A VALUE FROM 2 TO 8 INCLUSIVE. IT ALSO PROVIDES FOR NEW METHODS FOR MAKING COMPOUNDS USEFUL IN THE SYNTHESIS OF ZEARALANONE AND RELATED COMPOUNDS. THE NEW COMPOUNDS USEFUL AS INTERMEDIATES ARE 2,7-OCTADIENOIC ACID; METHYL 2,7-OCTADIENOATE; SODIUM ETHYL 6-(4-PENTENYL-B-DIHYDRORESORCYLATE; ETHYL 6-(4-PENTENYL)-B-DIHYDRORESORCYLATE; SODIUM METHYL 6-(4-PENTENYL)-B-DIHYDRORESORCYLATE; METHYL 6-(4-PENTENYL)-B-DIHYDRORESORCYLATE; METHYL 3-BROMO-6(4-PENTENYL)-B-DIHYDRORESORCYLATE; METHYL6-(4-PENTENYL9-B-RESORCYLATE; ETHYL 6-(4-PENTENYL)-B-RESORCYLATE; ETHYL 6-(4-PENTENYL)-B-R-RESORCYLATE DIBENZYL ESTER; TETRAHYDROJPYRAN-2-YL 4-YL 4-PENTEN-2-YL ETHER; ETHYL 6-(6-OXO-10-TETRAHYDROPYRAN-2-XYLOXYUNDECYL)-BRESORCYLATE DIBENZYL ETHER; AND 6-(10-HYDROXY-6-OXOUNDECYL)-B-RESORCYLIC ACID DIBENZYL ETHER. METHODS FOR PREPARING THESE INTERMEDIATES ARE ALSO DISCLOSED.
专利号:US-2023183177-A1 优先权日:2020-04-24 标题:Enantioselective chemo-enzymatic synthesis of optically active amino amide compounds 发明人:GRILL BIRGIT; WINKLER MARGIT; SCHWAB HELMUT; STROHMEIER GERNOT; DONSBACH KAI; WALDVOGEL SIEGFRIED R; ARNDT SEBASTIAN; WEIS DOMINIK 权利人:PHARMAZELL GMBH 摘要:The present invention relates to a novel biocatalytic process for the stereoselective preparation of alpha amino amide compounds catalyzed by NHase enzymes. A further aspect of the invention relates to novel NHase enzymes as well as further improved NHase enzyme mutants, nucleic acid molecules encoding these enzymes, recombinant microorganisms suitable for preparing such enzymes and mutants. Another aspect of the invention relates to a chemo-biocatalytic process for the preparation of lactam compounds comprising the new catalytic process for the preparation of alpha amino amide compounds catalyzed by NHase enzymes, as well as the chemical oxidation of the alpha amino amide by applying certain chemical oxidation catalysts suitable for converting the alpha amino amide under retention of its stereochemical configuration to the respective lactam. The novel chemo-biocatalytic process is particularly suited for the synthesis of valuable pharmaceutical compounds, like in particular (S)-Levetiracetam.
专利号:US-2023286918-A1 优先权日:2020-07-02 标 题:Manufacturing process for 3,5-dichloropicolinonitrile for synthesis of vadadustat 发明人:JURKAUSKAS VALDAS; JUNG YOUNG CHUN; KWON TAESOO; KANNAN ARUNACHALAM; GONDI VIJAYA BHASKER 权利人:AKEBIA THERAPEUTICS INC 摘要:Disclosed herein are methods and processes of preparing vadadustat or a pharmaceutically acceptable salts thereof, and intermediates (e.g., a compound of Formula (I), (I-F), (II), or (IV), or a pharmaceutically acceptable salts thereof) useful for the synthesis of vadadustat.
专利号:US-2008125587-A1 优先权日:2006-05-25 标 题 :Synthesis of triazole compounds that modulate HSP90 activity 发明人:CHIMMANAMADA DINESH U; LEE CHI-WAN; JAMES DAVID; ZHANG SHIJIE; YING WEIWEN; CHAE JUNGHYUN; PRZEWLOKA TERESA 权利人:CHIMMANAMADA DINESH U; LEE CHI-WAN; JAMES DAVID; ZHANG SHIJIE; YING WEIWEN; CHAE JUNGHYUN; PRZEWLOKA TERESA 摘要:The present invention provides novel methods of preparing triazole compounds which inhibit the activity of Hsp90. One embodiment of the invention is directed to methods for preparing a triazole compound represented by the following Structural Formula: n n n n n n n n n n or a tautomer, a pharmaceutically acceptable salt, solvate, or clathrate, or a prodrug thereof, comprising the steps of: a) reacting an amide represented by the following Structural Formula: n n n n n n n n n n with a thionation reagent to form a thioamide; b) reacting the thioamide of step a) with hydrazine to form a hydrazonamide; c) reacting the hydrazonamide of step b) with a carbonylation or a thiocarbonylation reagent. n In one embodiment, the present invention is a method of synthesis of a compound of formula (IA) n n n n n n n n n n or a tautomer, a pharmaceutically acceptable salt, solvate, or clathrate, or a prodrug thereof, comprising reacting a compound of formula (IIA) n n n n n n n n n n with an oxidizing agent, thereby producing a compound of formula (IA). n The present invention is also directed to a method of preparing a compound or a tautomer thereof represented by the following Structural Formula: n n n n n n n n n n or a tautomer, a pharmaceutically acceptable salt, solvate, or clathrate, or a prodrug thereof. The method comprises the step of reacting a first starting compound represented by the following Structural Formula: n n n n n n n n n n in the presence of a mercuric salt, with a second starting compound represented by the following Structural Formula:
专利号:US-7655769-B2 优先权日:2004-07-20 标题:Orthogonally protected disaccharide building blocks for synthesis of heparin 发明人:HUNG SHANG-CHENG; LEE JING-CHYI; LU XIN-AN 权利人:ACADEMIA SINICA 摘要:Orthogonally protected disaccharide building blocks for synthesis of heparin saccharide are disclosed. The disaccharide building block has a formula (I), in which L is a leaving group, P 1 , P 2 , P 3 and P 4 are different, and of them P 1 is an ester-type protecting group, P 2 is a hydroxyl protecting group that could be oxidized to a carboxylic acid, P 3 is a hydroxyl protecting group, and P 4 is a hydroxyl protecting group which allows chemoselective deprotection with 2,3-dichloro-5,6-dicyano-1,4-benzoquinone (DDQ). Acting as an elongation unit, the disaccharide building block of formula (I) may react with a starting unit of formula (II) to synthesize a heparin saccharide of desired size.
摘要:Merino, P., Science of Synthesis, (2010) 45, 304. 摘要:Kostikov, R. R.; Khlebnikov, A. F.; Sokolov, V. V., Science of Synthesis, (2010) 47, 774. 摘要:Kostikov, R. R.; Khlebnikov, A. F.; Sokolov, V. V., Science of Synthesis, (2010) 47, 777. 摘要:Kostikov, R. R.; Khlebnikov, A. F.; Sokolov, V. V., Science of Synthesis, (2010) 47, 848. 摘要:Kostikov, R. R.; Khlebnikov, A. F.; Sokolov, V. V., Science of Synthesis, (2010) 47, 816.