专利号:US-7619116-B2 优先权日:2003-12-17 标 题:Intermediates for the synthesis of (R)-tamsulosin and of its pharmaceutically acceptable salts and process for their preparation 发明人:DAMBRIN VALERY; LENOIR JEAN-YVES; SCHNEIDER JEAN-MARIE; GUILLAMOT GERARD; FOLLET MICHEL; BECKER ABRAM 权利人:PRODUCTS CHIMIQUES AUXILIAIRES 摘要:A subject matter of the present invention is novel intermediates for the synthesis of (R)-tamsulosin and of its pharmaceutically acceptable salts, and also the associated preparation process.
专利号:US-7098354-B2 优先权日:2002-10-25 标 题:Racemoselective synthesis of rac-diorganosilylbis(2-methylbenzo[e]indeyl)zirconium compounds 发明人:DAMRAU HANS-ROBERT; MUELLER PATRIK; GARCIA VALERIE; SIDOT CHRISTIAN; TELLIER CHRISTIAN; LELONG JEAN-FRANCOIS 权利人:BASELL POLYOLEFINE GMBH 摘要:The present invention relates to a specific process for the diastereoselective synthesis of rac-diorganosilylbis(2-methylbenzo[e]indenyl)zirconium compounds of the formula I, n nby reacting the silyl-bridged bisindenyl ligand with a dihalozirconium bis(3,5-di-tert-butylphenoxide)-base adduct to form the diorganosilylbis(2-methylbenzo[e]indenyl)zirconium bis(3,5-di-tert-butylphenoxide) and subsequently replacing the phenoxide groups by X using suitable replacement reagents to give the compound of the formula I; where the substituents X can be identical or different and are each F, Cl, Br, I or linear, cyclic or branched C 1-10 -alkyl; and the substituents R can be identical or different and are each linear, cyclic or branched C 1-10 -alkyl or C 6-10 -aryl; and also to the use of these compounds as catalysts.
专利号:US-6608196-B2 优先权日:2001-05-03 标题 :Process for solid supported synthesis of pyruvate-derived compounds 发明人:WANG BING; JANAGANI SATYANARAYANA; CALLAWAY WYETH B; SESSLER JONATHAN L 权利人:GALILEO PHARMACEUTICALS INC 摘要:Provided are processes for synthesizing structurally diverse pyruvate-derived compounds using a parallel approach on a solid phase support. Examples of such a solid phase support include resins which have also been used in solid phase peptide synthesis.
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-5157122-A 优先权日:1991-01-18 标 题 :Process for the preparation of 3-unsubstituted indoles using methane sulfonic acid as an additional catalyst 发明人:HUGHES DAVID L; ZHAO DALIAN 权利人:MERCK & CO INC 摘要:An indole having the formula I: I is prepared by a Fischer-Indole reaction employing a mixture of phosphorous pentoxide and methane sulfonic acid as an acid catalyst. The reaction, which is optionally run in a co-solvent, provides 3-unsubstituted indoles in high yields with high regioselectivity. The indole thus prepared is an intermediate in the synthesis of leukotriene biosynthesis inhibitors.
专利号:US-9045462-B2 优先权日:2012-08-17 标 题 :Synthesis of an antiviral compound 发明人:EVANS JARED WAYNE; FUJIMORI SHINJI; HUYNH GRACE M; LIU QI; TERESK MARTIN GERALD 权利人:GILEAD SCIENCES INC 摘要:The present disclosure provides processes for the preparation of a compound of Formula I: n nwhich is useful as an antiviral agent. The disclosure also provides compounds that are synthetic intermediates to compounds of formula.