专利号:US-2007293706-A1 优先权日:2004-11-01 标 题:Synthesis Of 1,5-Disubstituted-2-Hydroxy-Gibbatetraen-6-Ones 发明人:WILKENING ROBERT R; FRIED AMY; PARKER DANN L JR 权利人:WILKENING ROBERT R; FRIED AMY; PARKER DANN L JR 摘要:1,5-disubstituted-2-hydroxy-gibbatetraen-6-ones are useful as estrogen receptor modulators and as precursors to estrogen receptor modulators. The current invention provides a method for the synthesis of 1,5-disubstituted-2-hydroxy-gibbatetraen-6-ones from simple indanone starting materials via a Robinson-type annulation followed by an internal alkylation reaction. This invention further describes the novel use of a fluoroethyl substituent as a latent alkylating group for an internal cyclization reaction.
专利号:WO-9516653-A1 优先权日:1993-12-17 标 题 :Process for the synthesis of 1-bromo-2-fluoroethane 发明人:IIKUBO YUICHI; ZUBERI SHARIQUE S; BRANDSTADTER STEPHAN M; HEDRICK VICTORIA E; BORDEN DENNIS M 权利人:GREAT LAKES CHEMICAL CORP 摘要:A process for the bulk synthesis of 1-bromo-2-fluoroethane by reacting HBr and vinyl fluoride in the presence of an O2 catalyst in the liquid phase. More particularly, vinyl fluoride, hydrogen bromide and an O2 catalyst are dissovled in methylene chloride and mixed to form 1-bromo-2-fluoroethane.
专利号:US-9556140-B2 优先权日:2013-01-26 标 题 :Approach for synthesis of catechins 发明人:DUGAR SUNDEEP; MAHAJAN DINESH; RAI KUMAR SANTOSH; TRIPATHI VINAYAK; PATIL ISHWAR RAKESH 权利人:SPHAERA PHARMA PRIVATE LTD 摘要:A process for synthesis of enatiomerically pure or enatiomerically enriched or racemic mixture of (+ and/or −) epicatechin and its intermediates, comprising the steps of: (i) obtaining penta-protected quercetin; (ii) reducing the penta-protected quercetin obtained from step (i); (iii) optionally deprotecting the compound of step (ii); (iv) reducing the compound obtained from step (ii) or step (iii) in the presence of a chiral/achiral reducing agent to obtain a chiral intermediate; (v) deprotecting and/or hydrogenation of the chiral intermediate obtained from step (iv) to obtain (−)-epicatechin; (vi) optionally simultaneously deprotecting and by drogenation of the compound obtained from step (ii) to obtain racemic epicatechin.
专利号:US-6455680-B1 优先权日:2000-12-21 标 题 :Methods utilizing aryl thioimines in synthesis of erythromycin derivatives 发明人:LUKIN KIRILL A 权利人:ABBOTT LAB 摘要:An efficient deoximation technique for use in synthesis of erythromycin derivatives, involving aryl thioimine intermediates is disclosed. The aryl thioimine intermediates can be utilized in a method for protecting a ketone of a ketone-containing erythromycin derivative as a thioimine; a method for deoximating an oxime-containing erythromycin derivative, or a method for preparing a 6-O-alkyl erythromycin derivative. Presently preferred erythromycin derivatives have a C-9 oxime or a C-9 ketone.
专利号:US-8193360-B2 优先权日:2003-07-31 标 题:Radiolabelled fluorobenzamide analogues, their synthesis and use in diagnostic imaging 发明人:MACH ROBERT H; TU ZHUDE 权利人:MACH ROBERT H; TU ZHUDE; UNIV WASHINGTON 摘要:Fluoroalkoxybenzamide compounds which selectively bind Sigma-2 receptors are disclosed. These compounds, when labelled with 18 F, can be used as radiotracers for imaging of tumors by positron emission tomography (PET). In addition, these compounds, when labelled with 123 I, can be used as radiotracers for imaging of tumors by single photon emission computed tomography (SPECT). Methods for synthesis of these compounds are also disclosed.
专利号:US-9428482-B2 优先权日:2011-01-27 标 题 :Process for synthesis of polyphenols 发明人:DUGAR SUNDEEP; MAHAJAN DINESH; PANTELIS PETER GIANNOUSIS; SINGH VIJAY; KAPOOR KAMAL KISHORE 权利人:DUGAR SUNDEEP; MAHAJAN DINESH; PANTELIS PETER GIANNOUSIS; SINGH VIJAY; KAPOOR KAMAL KISHORE; SPHAERA PHARMA PTE LTD 摘要:The present invention provides synthetic processes for preparing racemic and/or optically pure epicatechin, epigallocatechin and related polyphenols as such or as their variously functionalized derivatives. A principle objective of the disclosure is to provide a new and useful method of synthesis to obtain polyphenols in isomerically pure and/or racemic forms.