专利号:US-6849743-B2 优先权日:1997-08-15 标 题 :Synthesis of clasto-lactacystin β-lactone and analogs thereof 发明人:SOUCY FRANCOIS; FLAMONDON LOUIS; BEHNKE MARK; ROUSH WILLIAM 权利人:MILLENNIUM PHARM INC 摘要:The present invention is directed to an improved synthesis of clasto-lactacystin-β-lactone, and analogs thereof, that proceeds in fewer steps and in much greater overall yield than syntheses described in the prior art. The synthetic pathway relies upon a novel stereospecific synthesis of an oxazoline intermediate and a unique stereoselective addition of a formyl amide to the oxazoline. Also described are novel clasto-lactacystin-β-lactones, and analogs thereof and their use as proteasome inhibitors.
专利号:US-2007260076-A1 优先权日:2003-12-05 标 题:Practical, Cost-Effective Synthesis of Ubiquinones 发明人:LIPSHUTZ BRUCE H; BERL VOLKER; SHEIN KARIN; WETTERICH FRANK 权利人:LIPSHUTZ BRUCE H; BERL VOLKER; SHEIN KARIN; WETTERICH FRANK 摘要:The present invention provides a convergent method for the synthesis of ubiquinones and ubiquinone analogues. Also provided are precursors of ubiquinones and their analogues that are useful in the methods of the invention. The invention further provides an improved method for the carboalumination of alkyne substrates.
专利号:US-2006167289-A1 优先权日:2003-12-05 标题 :Practical, cost-effective synthesis of ubiquinones 发明人:LIPSHUTZ BRUCE H; BERL VOLKER; SCHEIN KARIN; WETTERICH FRANK 权利人:ZYMES LLC 摘要:The present invention provides a convergent method for the synthesis of ubiquinones and ubiquinone analogues. Also provided are precursors of ubiquinones and their analogues that are useful in the methods of the invention. The invention further provides an improved method for the carboalumination of alkyne substrates.
专利号:US-2008039642-A1 优先权日:2004-09-23 标题 :Practical, Cost-Effective Synthesis of Chloromethylated 1, 4-Benzoquinones 发明人:BERL VOLKER; WETTERICH FRANK; ERNST HANSGEORG; SCHEIN KARIN 权利人:BERL VOLKER; WETTERICH FRANK; ERNST HANSGEORG; SCHEIN KARIN 摘要:The present invention relates to a practical and cost-effective method for the synthesis of 5-chloromethylated 2,3-dialkoxy-6-alkyl-1,4-benzoquinones by direct chloromethylation of the corresponding 2,3-dialkoxy-6-alkyl-1,4-benzoquinones. The invention further relates to a method for the preparation of 5-chloromethylated 2,3-dialkoxy-6-alkyl-1,4-benzoquinones starting from a 3,4,5-trialkoxy-1-alkyl-benzene. The invention also relates to a method for the production of Coenzymes Q n , especially coenzyme Q 10 .
专利号:US-2014323705-A1 优先权日:2011-05-13 标题:Manufacture of lacto-n-tetraose 发明人:HEDEROS MARKUS; DEKANY GYULA; DEMKÓ SÃ?NDOR; Kovács Imre; BAJZA ISTVÃ?N 权利人:HEDEROS MARKUS; DEKANY GYULA; DEMKÓ SÃ?NDOR; Kovács Imre; BAJZA ISTVÃ?N 摘要:The present invention relates to the synthesis of the tetrasaccharide of formula (I) and novel intermediates used in the synthesis.
专利号:US-11976081-B2 优先权日:2019-04-26 标题 :Intermediate of eribulin and synthesis method and use thereof 发明人:XU WEIPING 权利人:BEIJING TIENYI LUFU PHARMATECH CO LTD 摘要:An intermediate compound is prepared and used for the synthesis of halichondrin B, eribulin or an analog thereof, particularly a structural fragment C27-C35 thereof. The starting materials of the synthetic route are readily available, and the optical purity of the starting materials can be ensured, so that the optical purity of the structural fragment C27-C35 in halichondrin B, eribulin or the analog thereof is ensured. Steps for constructing a chiral center of the structural fragment C27-C35 feature higher diastereoselectivity and yield, in particular preparation methods of compounds of formulae (X), (XI), (XVI) and (XV). By-products of partial reactions can be removed only by recrystallization, which results in easy purification and significant reduce in cost.
[参考文献]: R G Hicks, Et Al. Spin Distributions, Ring Conformations, And Spiroconjugation In "Phosphaverdazyl" Radicals. Inorg Chem. 2001 Apr 9;40(8):1865-70.
合成参考文献
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