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-7816544-B2 优先权日:2004-03-23 标 题:Synthesis of rocaglamide natural products via photochemical generation of oxidopyrylium species 发明人:JONES II GUILFORD; GERARD BAUDOUIN; PORCO JR JOHN A 权利人:UNIV BOSTON 摘要:The present invention provides new strategies for the synthesis of compounds of the rocaglamide family and related natural products. In particular, the new biomimetic synthetic approach involves photochemical generation of an oxidopyrylium species from a 3-hydroxychromone derivative followed by 1,3-dipolar cycloaddition of the oxidopyrylium species to a dipolarophile. This approach can be used for the formation of adducts containing an aglain core structure. Methods for the conversion of aglain core structures to aglain, rocaglamide and forbaglin ring systems are also provided. The present invention also relates to the use of rocaglamide/aglain/forbaglin derivatives for the manufacture of medicaments for use in the treatment of cancer or cancerous conditions, disorders associated with cellular hyperproliferation, or NF-κB-dependent conditions.
专利号:US-8951728-B2 优先权日:2004-11-22 标 题:Template directed split and mix synthesis of small molecule libraries 发明人:RASMUSSEN PETER BIRK 权利人:CHEMGENE HOLDING APS 摘要:The invention combines the advantages of split and mix synthesis with the advantages of template directed synthesis. The method comprises the steps of: a) adding a linker molecule L to one or more reaction wells; b) adding a molecule fragment to each of said reaction wells; c) adding an oligonucleotide identifier to each of said reaction wells; d) subjecting said wells to conditions sufficient to allow said molecule fragments and said oligonucleotide identifiers to become attached to said linker molecule, or conditions sufficient for said molecule fragments to bind to other molecule fragments and sufficient for said oligonucleotide identifiers to bind to other oligonucleotide identifiers; e) combining the contents of said one or more reaction wells; and f) contacting the resulting bifunctional molecule(s) of step e) with one or more (oligonucleotide) templates each capable of hybridizing to at least one of the oligonucleotide identifiers added in step c).
专利号:US-6573387-B1 优先权日:1997-03-21 标 题 :Synthesis of α,β-substituted amino amides, esters, and acids 发明人:SHARPLESS K BARRY; RUBIN A ERIK 权利人:SCRIPPS RESEARCH INST 摘要:α,β-Unsaturated amides and esters are converted to α,β-substituted amino amides, esters, and acids. An α,βunsaturated amide or ester is first converted to an α,β-hydroxysulfonamide or hydroxycarbamate amide or ester using an osmium-catalyzed aminohydroxylation. The α,β-hydroxysulfonamide or hydroxycarbamate amides or esters is then cyclodehydrated to produce a α,β-N-sulfonyl- or the α,β-N-carbamoylaziridine amide or ester. The ring of aziridine intermediate is then nucleophilically opened in a regioselective manner with a variety of nucleophiles to give the $g(α,β-substituted amino- amides or esters. Preferred nucleophiles include sulfur, oxygen, carbon, and nitrogen nucleophiles.
专利号:WO-2014012832-A1 优先权日:2012-07-16 标 题:Process for the preparation of 2-(3-n,n-diisopropylamino-1-phenylpropyl)-4-hydroxymethyl-phenol and its derivatives 发明人:PICCOLO ORESTE; GIANNINI ELIOS; BIGINI LAURA; GIANOLLI EDOARDO; VIGO DANIELE 权利人:CAMBREX PROFARMACO MILANO S R L 摘要:The invention concerns a process for the preparation of 2-(3-N,N- diisopropylamino-l-phenylpropyl)-4-hydroxymethyl-phenol and its derivatives, particularly the corresponding (R) 4-trityloxymethyl derivative, useful as intermediate form in the synthesis of Fesoterodine and its salts, in particular for the preparation of Fesoterodine fumarate salt.
参考文献:10.1021/jo0604686 摘要:Takahashi H, Takashima Y, Yamaguchi H, Harada A. Selection between pinching-type and supramolecular polymer-type complexes by alpha-cyclodextrin-beta-cyclodextrin hetero-dimer and hetero-cinnamamide guest dimers. J Org Chem. 2006 Jun 23;71(13):4878–83. doi: 10.1021/jo0604686. 参考文献:10.1080/10286020290011396 摘要:Zhou L, Ding Y. A cinnamide derivative from solanum verbascifolium L. Journal of Asian Natural Products Research. 2002 Jan;4(3):185–7. doi: 10.1080/10286020290011396. 参考文献:10.1016/j.bmcl.2006.08.055 摘要:Li YH, Coppo FT, Evans KA, Graybill TL, Patel M, Gale J, Li H, Tavares F, Thomson SA. Synthesis and structure–activity relationships of 3-phenyl-2-propenamides as inhibitors of glycogen phosphorylase a. Bioorganic & Medicinal Chemistry Letters. 2006 Nov;16(22):5892–6. doi: 10.1016/j.bmcl.2006.08.055. 参考文献:10.1016/j.bmcl.2010.01.031 摘要:Bairwa R, Kakwani M, Tawari NR, Lalchandani J, Ray MK, Rajan MGR, Degani MS. Novel molecular hybrids of cinnamic acids and guanylhydrazones as potential antitubercular agents. Bioorganic & Medicinal Chemistry Letters. 2010 Mar;20(5):1623–5. doi: 10.1016/j.bmcl.2010.01.031.