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:WO-2025108575-A1 优先权日:2023-11-21 标 题:Methods of selective deprotection and synthesis of transhydrindane- skeleton-based compounds 发明人:HUBER FLORIAN MAURITIUS ERASMUS 权利人:ROCHE DIAGNOSTICS GMBH 摘要:The present invention relates to methods of selectively deprotecting a transhydrindane-skeleton-based compound comprising at least two different silyl ether groups. The present invention further relates to methods of synthesizing a Vitamin D molecule and to Vitamin D molecules obtainable by such processes. Furthermore, the present invention relates to a compound according to formula (I) comprising two different silyl ether groups, its use in the synthesis of Vitamin D molecules and to methods of producing such a compound.
专利号:WO-9747313-A1 优先权日:1996-06-10 标题:Total synthesis of bacitracin polypetides 发明人:GRIFFIN JOHN H; MCDOUGAL PATRICK G 权利人:UNIV LELAND STANFORD JUNIOR 摘要:Methods for the total synthesis of bacitracin-type polypeptides are described, as well as useful analogs of bacitracin A, and treatment of bacterial infection using such analogs.
专利号:US-6342619-B2 优先权日:1999-04-01 标题:Synthesis of conjugated fatty acid 发明人:SEIDEL MICHAEL C 摘要:A synthesis process is disclosed for producing a conjugated fatty acid at specified temperature in high yield, including providing an ester of a fatty acid having somewhere in its carbon chain a chain of four carbon atoms such that carbon one bears one hydrogen and one hydroxyl group, carbon two bears two hydrogen atoms, and a double bond is positioned between carbon three and carbon four and reacting with a chloride selected from the group consisting of toluenesulfonyl chloride, methanesulfonyl chloride, benzenesulfonyl chloride, alkylsulfonyl chloride, and arylsulfonyl chloride at a temperature in the range of 10° C.-100° C., preferably 20° C.-50° C. The synthesis process provides a conjugated fatty acid formed from the ester reacted with diazabicycloundecene. In one aspect, the ester is formed in a pyridine solvent. In one aspect, a mesylate is formed with mesyl chloride in acetonitrile and triethyl amine. In one aspect, the reaction with diazabicyclo-undecene is conducted in a polar, non-hydroxylic solvent of acetonitrile to form a preferred isomer at the specified temperature in high yield.
专利号:US-6160141-A 优先权日:1997-02-18 标 题 :Synthesis of conjugated eicosadienoic acid 发明人:SEIDEL MICHAEL C 摘要:A synthesis process for producing 11-cis, 13-trans eicosadienoic acid at room temperature in high yield is disclosed, including providing a tosylate or mesylate of a methyl lesquerolate and 11-cis, 13-trans eicosadienoic acid formed when the tosylate or mesylate reacts with diazabicyclo-undecene. In one aspect, the tosylate of the methyl lesquerolate is formed with tosyl chloride in a pyridine solvent. In one aspect, the mesylate of the methyl lesquerolate is formed with mesyl chloride in acetonitrile and triethyl amine. In one aspect, the tosylate or mesylate is reacted with diazabicyclo-undecene in a polar, non-hydroxylic solvent of acetonitrile to form the preferred isomer of 11-cis, 13-trans eicosadienoic acid at room temperature in high yield.
专利号:US-5892074-A 优先权日:1997-02-18 标 题:Synthesis of conjugated linoleic acid (CLA) 发明人:SEIDEL MICHAEL C 摘要:A synthesis process for producing 9-cis, 11-trans octadecadienoic acid at room temperature in high yield is disclosed, including providing a tosylate or mesylate of a methyl ester of ricinoleic acid and 9-cis, 11-trans octadecadienoic acid formed when the tosylate or mesylate reacts with diazabicyclo-undecene. In one aspect, the tosylate of the methyl ester of ricinoleic acid is formed with tosyl chloride in a pyridine solvent. In one aspect, the mesylate of the methyl ester of ricinoleic acid is formed with mesyl chloride in acetonitrile and triethyl amine. In one aspect, the tosylate or mesylate is reacted with diazabicyclo-undecene in a polar, non-hydoxylic solvent of acetonitrile to form the preferred isomer of 9-cis, 11-trans octadecadienoic acid at room temperature in high yield.
摘要:de Meijere, A., Science of Synthesis, (2010) 47, 1. 摘要:Schramm, M. P., Science of Synthesis, (2009) 46, 448. 摘要:Schramm, M. P., Science of Synthesis, (2009) 46, 508. 摘要:Kostikov, R. R.; Khlebnikov, A. F.; Sokolov, V. V., Science of Synthesis, (2010) 47, 816. 摘要:Kubik, S., Science of Synthesis Knowledge Updates, (2013) 3, 265.