专利号:US-8329958-B2 优先权日:2004-07-02 标 题:Combinatorial synthesis of PEG oligomer libraries 发明人:RIGGS-SAUTHIER JENNIFER A; EKWURIBE NNOCHIRI N 权利人:RIGGS-SAUTHIER JENNIFER A; EKWURIBE NNOCHIRI N; BIOCON LTD 摘要:A simple chain-extending approach was established for the scale-up of the monoprotected monodisperse PEG diol materials. Reactions of THP-(OCH2CH2)n—OMs (n=4, 8, 12) with a large excess of commercially available H—(OCH2CH2)n—OH (n=1-4) under basic conditions led to THP-(OCH2CH2)n—OH (n=5-15). Similarly, Me-(OCH2CH2)n—OH (n=4-11, 13) were prepared from Me-(OCH2CH2)n—OMs (n=3, 7, 11). For the chain elongation steps, 40-80% yields were achieved through extraction purification. PEG oligomer libraries I and II were generated in 50-95% overall yields by alkylation or acylation of THP-(OCH2CH2)n—OH (n=1-15) followed by deprotection. Alkylation of Me-(OCH2CH2)n—OH (n=1-11, 13) with X—(CH2)m—CO2R (X=Br or OMs) and subsequent hydrolysis led to PEG oligomer library III in 30-60% overall yields. Combinatorial purification techniques were adapted to the larger-scale library synthesis. A total of 498 compounds, each with a weight of 2-5 g and a minimum purity of 90%, were synthesized.
专利号:US-5756790-A 优先权日:1995-09-29 标题 :Optically active cobalt (II) complexes and method for the preparation of optically active alcohols 发明人:MUKAIYAMA TERUAKI; YOROZU KIYOTAKA; NAGATA TAKUSHI; YAMADA TORU; SUGI KIYOAKI 权利人:MITSUI PETROCHEMICAL IND 摘要:The invention provides a method for preparing an optically active alcohol comprising the step of reacting a ketone compound with a hydride reagent in the presence of an optically active metal compound. The resulting optically active alcohols are useful as intermediates for the synthesis of physiologically active compounds such as drugs and pesticides, functional materials such as liquid crystals, and raw materials for synthesis in fine chemistry. A novel optically active cobalt (II) complex useful as a catalyst is also provided.
专利号:WO-0078725-A1 优先权日:1999-06-18 标题 :Synthesis of substituted amidines 发明人:CHOUEIRY DANIELE; GIRAUD DANIEL LIONEL; SCHOTTEN THEO 权利人:LILLY CO ELI; CHOUEIRY DANIELE; GIRAUD DANIEL LIONEL; SCHOTTEN THEO 摘要:The present invention provides a process for preparing amidines starting from carboxylic acid derivatives, in which the carboxylic acid containing moiety is attached to a sp3-, or sp?2- or sp1¿-hybridized carbon atom. The sp2-hybridized carbon atom, to which the carboxylic acid containing moiety is attached to may be part of an aromatic or heteroaromatic or olefinic system.
专利号:US-4866188-A 优先权日:1984-08-03 标 题 :Synthesis of cyclic ethers 发明人:SCHEBEN JOHN A 权利人:NAT DISTILLERS CHEM CORP 摘要:A process is disclosed for preparing a cyclic ether which comprises cyclodehydrating a polyhydroxy compound of the general formula n n HOR.sup.1 HC--R.sup.2 --CHR.sup.3 OH n n in which R 1 and R 3 , each of which is the same or different, is hydrogen or a lower aliphatic, cycloaliphatic or aryl group and R 2 is a divalent aliphatic group of 1 to 10 carbon atoms containing 0, 1 or 2 etheric oxygen atoms or 0, 1 or 2 secondary or tertiary amine nitrogen atoms and 0, 1 or more lower aliphatic, cycloaliphatic and/or aryl groups containing 0 or 1 hydroxyl groups at elevated temperatures in the presence of a catalytically effective amount of a Group VIII metal catalyst or a Group VIII metal-containing material to provide a cyclic ether of the general formula ##STR1## in which R 1 , R 2 and R 3 are as defined above. The process is especially useful for preparing the commercially important cyclic ethers tetrahydrofuran and 1,4-dioxane which are derived from 1,4-butanediol and ethylene glycol and/or diethylene glycol, respectively.
专利号:US-8487108-B2 优先权日:2005-11-14 标题 :Piperidinyl carbamate intermediates for the synthesis of aspartic protease inhibitors 发明人:BALDWIN JOHN J; CLAREMON DAVID A; TICE COLIN; CACATIAN SALVACION; DILLARD LAWRENCE W; ISHCHENKO ALEXEY V; YUAN JING; XU ZHENRONG; MCGEEHAN GERARD; SIMPSON ROBERT D; SINGH SURESH B; ZHAO WEI; FLAHERTY PATRICK T 权利人:BALDWIN JOHN J; CLAREMON DAVID A; TICE COLIN; CACATIAN SALVACION; DILLARD LAWRENCE W; ISHCHENKO ALEXEY V; YUAN JING; XU ZHENRONG; MCGEEHAN GERARD; SIMPSON ROBERT D; SINGH SURESH B; ZHAO WEI; FLAHERTY PATRICK T; VITAE PHARMACEUTICALS INC 摘要:The present invention is directed to aspartic protease inhibitors. Certain aspartic protease inhibitors of the invention can be represented by the following structural formula or a pharmaceutically acceptable salt thereof. The present invention is also directed to pharmaceutical compositions comprising the disclosed aspartic protease inhibitors. The present invention is further directed to methods of antagonizing one or more aspartic proteases in a subject in need thereof, and methods for treating an aspartic protease mediated disorder in a subject using the disclosed aspartic protease inhibitors.
专利号:US-5637757-A 优先权日:1995-04-11 标 题 :One-pot synthesis of ring-brominated benzoate compounds 发明人:HILL JOHN E; FAVSTRITSKY NICOLAI A; MAMUZIC RASTKO I; BHATTACHARYA BHABATOSH 权利人:GREAT LAKES CHEMICAL CORP 摘要:A method of preparing tetrabromobenzoate compounds from tetrabromophthalic anhydride by reacting tetrabromophthalic anhydride with alcohol in the presence of a decarboxylation catalyst. The reaction may be carried out in an excess of alcohol, or with a near stoichiometric amount of alcohol by performing the reaction in an inert solvent.