葑酮置于copper Chromite,氢气体系中,用 甲醇 用作溶剂,175.0 °C,19.99 Mpa 条件下,反应 19.0H,反应生成葑醇 参考文献:High Potency Dipeptide Sweeteners. 1. L-Aspartyl-D-Phenylglycine Esters 标题:High Potency Dipeptide Sweeteners. 1. L-Aspartyl-D-Phenylglycine Esters 摘要:Twenty Esters Of L-Aspartyl-D-Phenylglycine,As Well As Two Substituted Analogues,An O-Fluoro And A P-Hydroxy-Phenylglycine Ester,Were Prepared. The L-Aspartyl-D-Phenylglycine (-)-Alpha-And (+)-Beta-Fenchyl Esters Had The Highest Sweetness Potency At 1200 And 3700 Times That Of Sucrose,Respectively. The High Potency Of These Sweeteners Is Surprising As The Phenyl Group occupies A Position Previously Believed To Accommodate Only Much Smaller Groups. Doi:10.1021/jm00165A027
专利号:US-8198465-B2 优先权日:2005-10-17 标 题 :3-alkyl-5- (4-alkyl-5-oxo-tetrahydrofutran-2-yl) pyrrolidin-2-one derivatives as intermediates in the synthesis of renin inhibitors 发明人:SEDELMEIER GOTTFRIED; GRIMLER DOMINIQUE; ACEMOGLU MURAT 权利人:SEDELMEIER GOTTFRIED; GRIMLER DOMINIQUE; ACEMOGLU MURAT; NOVARTIS AG 摘要:The invention related to a novel process, novel process steps and novel intermediates useful in the synthesis of pharmaceutically active compounds, especially renin inhibitors, such as Aliskiren. Inter alia, the invention relates to a process for the manufacture of a compound of the formula II, n nor a salt thereof, and a compound of formula VIn n nor a salt thereof, wherein R 3 and R 4 as well as Act are as defined in the specification, and processes of manufacturing these.n n Additionally transformation of compounds (VI) with metallo organic compounds (VII) give rise to the new compounds (VIII) which are direct precursors for the preparation of Aliskiren.
专利号:US-7462738-B2 优先权日:2006-05-24 标题:Processes for the preparation of R-(+)-3-(carbamoyl methyl)-5-methylhexanoic acid and salts thereof 发明人:HEDVATI LILACH; GILBOA EYAL; AVHAR-MAYDAN SHARON 权利人:TEVA PHARMA 摘要:Provided are processes for the synthesis of R-(+)-3-(carbamoylmethyl)-5-methylhexanoic acid and salts thereof, intermediates in the synthesis of S-pregabalin.
专利号:US-2021206711-A1 优先权日:2020-01-03 标 题:Synthesis of the Grape Mealybug Pheromone trans-alpha-Necrodyl Isobutyrate 发明人:CHEBNY VINCENT JAMES 权利人:TRECE INC 摘要:Methods are provided for synthesizing the grape mealybug pheromone, trans-α-necrodyl isobutyrate, starting with essential plant oils that contain trans-α-necrodyl acetate. The synthesis method, in two steps, converts the trans-α-necrodyl acetate to trans-α-necrodol and then converts the trans-α-necrodol to the desired trans-α-necrodyl isobutyrate. The first step can be achieved by either of a hydrolysis reaction or a reduction reaction. In the hydrolysis reaction, the essential oil is mixed in an alcohol solvent with a hydroxide base, or by mixing the essential oil in an aqueous acid. A reduction reaction can instead by performed in an organic solvent in the presence of a reducing agent. The trans-α-necrodol is converted to the desired trans-α-necrodyl isobutyrate by an esterification reaction with a carboxylic acid, an acyl halide, or an acid anhydride.
专利号:US-7635783-B2 优先权日:2003-12-19 标题 :Meso-selective synthesis of ansa-metallocenes 发明人:CHEVALIER REYNALD; MUELLER PATRIK; SIDOT CHRISTIAN; TELLIER CHRISTIAN; GARCIA VALERIE; DELANCRAY LUDOVIC 权利人:BASELL POLYOLEFINE GMBH 摘要:The present invention relates to a process for the meso-selective preparation of ansa-metallocene complexes of the formula (I), which comprises reacting a ligand starting compound of the formula (II) with a transition metal compound of the formula III, where R 1 , R 1 are identical or different and are each hydrogen or an organic radical having from 1 to 40 carbon atoms, R 2 , R 2 are identical or different and are each hydrogen or an organic radical having from 1 to 40 carbon atoms, R 3 is a bulky organic radical which has at least 3 carbon atoms, is bound to the oxygen atom via a nonaromatic carbon or silicon atom and may be substituted by halogen atoms or further organic radicals having from 1 to 20 carbon atoms and may also contain heteroatoms selected from the group consisting of Si, N, P, O and S, T, T′ are identical or different and are each a divalent organic group which has from 1 to 40 carbon atoms and together with the cyclopentadienyl ring forms at least one further saturated or unsaturated, substituted or unsubstituted ring system having a ring size of from 5 to 12 atoms, where T and T′ may contain the heteroatoms Si, Ge, N, P, As, Sb, O, S, Se or Te within the ring system fused to the cyclopentadienyl ring, A is a bridge consisting of a divalent atom or a divalent group, M 1 is an element of group 3, 4, 5 or 6 of the Periodic Table of the Elements or the lanthanides, the radicals X are identical or different and are each an organic or inorganic radical which is able to be replaced by a cyclopentadienyl anion, x is a natural number from 1 to 4, M 2 is an alkali metal, an alkaline earth metal or a magnesium monohalide fragment, p is 1 in the case of doubly positively charged metal ions or 2 in the case of singly positively charged metal ions or metal ion fragments, LB is an uncharged Lewis base ligand, and y is a natural number from 0 to 6, and also the subsequent reaction of these complexes to form ansa-metallocenes of the formula (IV), the use of transition metal compounds of the formula (III) for preparing metallocenes and also transition metal compounds of the formula (III), ansa-metallocene complexes of the formula (I) and the use of these as constituents of catalyst systems for the polymerization of olefines.
专利号:US-5629394-A 优先权日:1992-12-17 标 题 :Direct synthesis by living cationic polymerization of nitrogen-containing polymers 发明人:CHERADAME HERVE M; CHEN FRANK J; STANAT JON E R; NGUYEN HUNG A; TABAR BEHROOZ R 权利人:EXXON CHEMICAL PATENTS INC 摘要:A method is provided for the direct synthesis by living cationic polymerization of novel polymeric materials functionalized with desirable nitrogen-containing functional groups such as terminal azido, cyano, carbonylamino, cyanato, thiocyanato or thiocarbonylamino groups. Polymerization and functionalization occur in a substantially simultaneous manner. All necessary reactants for the functionalization are present when polymerization is initiated. The nitrogen-containing functional group is provided as a part of a molecule having a release moiety which is preferably resonance stabilized or a tertiary alkyl type and which acts to aid the nitrogen-containing species in functioning as a leaving group.
专利号:US-2004053999-A1 优先权日:1997-09-17 标题 :Novel compounds and methods for synthesis and therapy 发明人:BISCHOFBERGER NORBERT W; DAHL TERRENCE C; HITCHCOCK MICHAEL J M; KIM CHOUNG U; LEW WILLARD; LIU HONGTAO; MILLS ROGER G; WILLIAMS MATTHEW A 摘要:Novel compounds are described. The compounds generally comprise an acidic group, a basic group, a substituted amino or N-acyl and a group having an optionally hydroxylated alkane moiety. Pharmaceutical compositions comprising the inhibitors of the invention are also described. Methods of inhibiting neuraminidase in samples suspected of containing neuraminidase are also described. Antigenic materials, polymers, antibodies, conjugates of the compounds of the invention with labels, and assay methods for detecting neuraminidase activity are also described.
摘要:Hari, Y.; Aoyama, T.; Shioiri, T., Science of Synthesis Knowledge Updates, (2010) 4, 60. 摘要:Zhang, Q.-W.; An, K.; He, W., Science of Synthesis Knowledge Updates, (2020) 3, 2. 摘要:Kashemirov, B. A.; Błażewska, K.; Justyna, K.; Lyu, J.; McKenna, C. E., Science of Synthesis Knowledge Updates, (2021) 1, 488. 参考文献:10.1080/14786419.2015.1094802 摘要:Salim M, Kabeer TKA, Nair SA, Dan M, Sabu M, Baby S. Chemical profile, antiproliferative and antioxidant activities of rhizome oil of Zingiber anamalayanum from Western Ghats in India. Natural Product Research. 2015 Oct 09;30(17):1965–8. doi: 10.1080/14786419.2015.1094802.