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-5801247-A 优先权日:1997-01-23 标题 :Process for the enantioselective synthesis of hydroxypyrrolidines from amino acids and products thereof 发明人:DALTON DAVID R; HUANG YIFANG 权利人:UNIV TEMPLE 摘要:The present invention relates to processes for the enantioselective synthesis of hydroxypyrrolidines from amino acids. An amino methyl ester is used as the starting material. The ester is reacted with a benziminoethyl ether to produce an oxazoline or thiazoline. Specifically, L-serine methyl ester is used to produce 4-(carbomethoxy)-2-phenyl-.increment. 2 -oxazoline, and cysteine is used to produce the corresponding thiazoline. The oxazoline (or thiazoline) can be reduced to an aldehyde by treatment with a slight excess of DIBAL-H. The oxazoline is quenched with alcohol and reacted with (carbomethoxymethylene)triphenylphosphorane, to produce (S)-(+)-methyl (E)- and (S)-(-)-methyl (Z)-3-(4,5-dihydro-2-phenyl-4-oxazolyl)-2-propenoate. The double bond is hydroxylated to yield the diol esters. The resulting diol is then treated with aqueous acid to hydrolyze the oxazoline and recyclize to produce 3,4-dihydroxy-5-hydroxymethylpyrrolidone benzoate. This is treated with an excess of borane in tetrahydrofuran to yield (2-hydroxymethyl) 3,4-dihydroxypyrrolidine. The intermediate compounds are useful both in the present process and as final products themselves. The total yield of the mixture of isomers, as well as their ratio, can be varied.
专利号:US-7491520-B2 优先权日:2004-01-19 标题 :Biochemical synthesis of 6-amino caproic acid 发明人:RAEMAKERS-FRANKEN PETRONELLA C; NOSSIN PETRUS M M; BRANDTS PAUL M; WUBBOLTS MARCEL G; PEETERS WIJNAND P H; ERNSTE SANDRA; WILDEMAN DE STEFAAN M A; SCHUERMANN MARTIN 权利人:DSM IP ASSETS BV 摘要:The invention relates to biochemical synthesis of 6-amino caproic acid from 6-aminohex-2-enoic acid compound or from 6-amino-2-hydroxyhexanoic acid, by treatment with an enzyme having α,β-enoate reductase activity towards molecules containing an α,β-enoate group and a primary amino group. The invention also relates to processes for obtaining suitable genetically engineered cells for being used in such biotransformation process, and to precursor fermentation of 6-amino caproic acid from intermediates leading to 6-amino caproic acid. Finally, the invention relates to certain novel biochemically produced compounds, namely 6-aminohex-2-enoic acid, 6-aminohexanoic acid, as well as to caprolactam produced therefrom and to nylon-6 and other derivatives produced from such biochemically produced compounds or caprolactam.
专利号:US-3681428-A 优先权日:1968-10-24 标 题:Synthesis of phosphorane compounds 发明人:ROBERTS DONALD LEROY; RICE WILLIAM YATES JR 权利人:REYNOLDS TOBACCO CO R 摘要:Synthesis of phosphorane compounds by reaction of a triarylphosphine, an Alpha -haloester and an amine.
专利号:US-2010022767-A1 优先权日:2008-07-25 标题 :Development of a synthesis of syringolin a and b and derivatives thereof 发明人:KAISER MARKUS; CLERC JEROME 权利人:MAX PLANCK GESELLSCHAFT 摘要:The synthesis of syringolin A and B and derivatives thereof as well as to pharmaceutical compositions containing the syringolin A or B or derivatives thereof and the use of syringolin A and B and derivatives thereof for prophylaxis and treatment of cancer.
专利号:US-5338865-A 优先权日:1992-03-12 标 题 :Synthesis of halichondrin B and norhalichondrin B 发明人:KISHI YOSHITO; FANG FRANCIS; FORSYTH CRAIG J; SCOLA PAULA M; YOON SUK KYOON 权利人:HARVARD COLLEGE 摘要:Novel chemical compounds that can be used to synthesize halichondrin B and norhalichondrin B, and related derivatives, are described. The synthesis of halichondrin B and norhalichondrin B from these compounds also is described.
摘要:Abell, A. D.; Edmonds, M. K., Science of Synthesis, (2009) 46, 25. 摘要:Abell, A. D.; Edmonds, M. K., Science of Synthesis, (2009) 46, 35. 摘要:Krause, N.; Arisetti, N., Science of Synthesis Knowledge Updates, (2020) 3, 101. 摘要:Kwiecień, H., Science of Synthesis Knowledge Updates, (2014) 4, 246. 摘要:Koutentis, P. A.; Ioannidou, H. A., Science of Synthesis Knowledge Updates, (2010) 1, 313.