专利号:US-6794534-B2 优先权日:2000-06-23 标题:Synthesis of functionalized and unfunctionalized olefins via cross and ring-closing metathesis 发明人:GRUBBS ROBERT H; CHATTERJEE ARNAB K; MORGAN JOHN P; SCHOLL MATTHIAS; CHOI TAE-LIM 权利人:CALIFORNIA INST OF TECHN 摘要:The invention is directed to the cross-metathesis and ring-closing metathesis reactions between geminal disubstituted olefins and terminal olefins, wherein the reaction employs a Ruthenium or Osmium metal carbene complex. Specifically, the invention relates to the synthesis of α-functionalized or unfunctionalized olefins via intermolecular cross-metathesis and intramolecular ring-closing metathesis using a ruthenium alkylidene complex. The catalysts preferably used in the invention are of the general formula n wherein: n M is ruthenium or osmium; n X and X 1 are each independently an anionic ligand; n L is a neutral electron donor ligand; and, n R, R 1 R 6 , R 7 , R 8 , and R 9 are each independently hydrogen or a substituent selected from the group consisting of C 1 -C 20 alkyl, C 2 -C 20 alkenyl, C 2 -C 20 alkynyl, aryl, C 1 -C 20 carboxylate, C 1 -C 20 alkoxy, C 2 -C 20 alkenyloxy, C 2 -C 20 alkynyloxy, aryloxy, C 2 -C 20 alkoxycarbonyl, C 1 -C 20 alkylthio, C 1 -C 20 alkylsulfonyl and C 1 -C 20 alkylsulfinyl.
专利号:US-2004242897-A1 优先权日:2002-07-31 标题 :Universal support media for synthesis of oligomeric compounds 发明人:GUZAEV ANDREI P; MANOHARAN MUTHIAH 摘要:Compounds for the synthesis of oligomeric compounds, particularly oligonucleotides and oligonucleotide mimetics, are provided. In addition, methods for functionalizing a support medium with a first monomeric subunit and methods for the synthesis of oligomeric compounds utilizing the novel compounds bound to support media are provided.
专利号:US-2004018598-A1 优先权日:2000-05-30 标题 :Bio-intermediates for use in the chemical synthesis of polyketides 发明人:SANTI DANIEL; ASHLEY GARY; MYLES DAVID C 摘要:The present invention relates to compounds made by a subset of modules from one or more polyketide synthase (“PKSâ€?) genes that are used as starting material in the chemical synthesis of novel molecules, particularly naturally occurring polyketides or derivatives thereof. The biologically derived intermediates (“bio-intermediatesâ€?) generally represent particularly difficult compounds to synthesize using traditional chemical approaches due to one or more stereocenters. In one aspect of the invention, an intermediate in the synthesis of epothilone is provided that feeds into the synthetic protocol of Danishefsky and co-workers. In another aspect of the invention, intermediates in the synthesis of discodermolide are provided that feed into the synthetic protocol of Smith and co-workers. By taking advantage of the inherent stereochemical specificity of biological processes, the syntheses of key intermediates and thus the overall syntheses of compounds like epothilone and discodermolide are greaty simplified.
专利号:US-2012215002-A1 优先权日:2009-10-09 标 题:Synthesis of optically active intermediate for the preparation of montelukast 发明人:LEFORT LAURENT 权利人:LEFORT LAURENT 摘要:The present invention relates to the synthesis of optically active alcohols by means of enantioselective hydrogenation of ketones in biphasic systems. In particular the present invention relates to the synthesis of an optically active alcohol of general formula (1).
专利号:US-2006287520-A1 优先权日:2005-05-16 标 题 :Synthesis of salinosporamide A and analogues thereof 发明人:DANISHEFSKY SAMUEL J; ENDO ATSUSHI 权利人:DANISHEFSKY SAMUEL J; ENDO ATSUSHI 摘要:A novel synthesis of salinosporamide A is provided. Salinospoamide A as well as structurally related natural products, omuralide and lactacystin, have been shown to be proteasome inhibitors. Therefore, these compounds as well as analogues of these natural products may be useful in the treatment of proliferative diseases such as cancer, autoimmune diseases, diabetic retinopathy, etc. The invention provides for the synthesis of salinosporamide A as well as analogs thereof using a convenient point for derivatization of the bicyclic core. Pharmaceutical compositions and method of using the inventive compounds are also provided.
专利号:US-7910623-B2 优先权日:2005-07-22 标 题 :Synthesis of scabronines and analogues thereof 发明人:DANISHEFSKY SAMUEL J; WATERS STEPHEN P 权利人:SLOAN KETTERING INST CANCER 摘要:A novel synthesis of scabronines, which are related to a broader class of angularly fused tricyclic diterpenoids known as cyathanes, is provided. Scabronine G, its methyl ester derivative, and other analogs have been shown to have neurotrophic activity. Therefore, these compounds are particularly useful in treating neurodegenerative diseases such as Alzheimer's disease, Parkinson's disease, Huntington's diseases, etc. The invention provides for the synthesis of scabronines as well as analogs thereof. Pharmaceutical compositions and method of using the inventive compounds are also provided.
参考文献:10.1177/112972981001100211 摘要:Thermann F, Wollert U, Ukkat J, Dralle H. Proximalization of the arterial inflow (PAI) in patients with dialysis access-induced ischemic syndrome: first report on long-term clinical results. J Vasc Access. 2010 Apr;11(2):143–9. doi: 10.1177/112972981001100211. 参考文献:10.18632/aging.100103 摘要:Krishnan N, Kretzschmar D, Rakshit K, Chow E, Giebultowicz JM. The circadian clock gene period extends healthspan in aging Drosophila melanogaster. Aging (Albany NY). 2009 Nov 19;1(11):937–48. 参考文献:10.18632/aging.100005 摘要:Singh SP, Niemczyk M, Zimniak L, Zimniak P. Fat accumulation in Caenorhabditis elegans triggered by the electrophilic lipid peroxidation product 4-hydroxynonenal (4-HNE). Aging (Albany NY). 2008 Dec 18;1(1):68–80. 参考文献:10.3290/j.jad.a17549 摘要:Nakayama D, Koizumi H, Komine F, Blatz MB, Tanoue N, Matsumura H. Adhesive bonding of zirconia with single-liquid acidic primers and a tri-n-butylborane initiated acrylic resin. J Adhes Dent. 2010 Aug;12(4):305–10. doi: 10.3290/j.jad.a17549. 参考文献:10.1007/s00425-010-1112-2 摘要:Yamauchi Y, Sugimoto Y. Effect of protein modification by malondialdehyde on the interaction between the oxygen-evolving complex 33 kDa protein and photosystem II core proteins. Planta. 2010 Apr;231(5):1077–88. doi: 10.1007/s00425-010-1112-2.