专利号:US-4049710-A 优先权日:1976-02-24 标题:Novel carbamimidoyl chlorides and their use in the synthesis of herbicidal triazinediones 发明人:TOCKER STANLEY 权利人:DU PONT 摘要:Carbamimidoyl chlorides of the formula: WHERE R2 is alkyl of 1-4 carbon atoms are useful as intermediates in the synthesis of herbicidal triazinediones of the formula: where R1 is certain organic radicals.
专利号:US-7034096-B2 优先权日:2002-02-19 标题:Ring-expansion of cyclic olefins metathesis reactions with an acyclic diene 发明人:CHOI TAE-LIM; LEE CHOON WOO; KIM HYUNJIN M; GRUBBS ROBERT H 权利人:CALIFORNIA INST OF TECHN 摘要:This invention relates generally to synthetic procedures that include the step of ring-opening metathesis of cyclic olefins and reaction with an acyclic diene co-reactant to produce olefin macrocycles by ring expansion, or alternatively. The ring expansion of the cyclic olefin is provided by three types of sequential olefin metathesis (ring-opening, cross, and ring-closing olefin metathesis). More particularly, the invention pertains to synthesis of olefin macrocycles via olefin metathesis reactions using a Group 8 transition metal complex as the metathesis catalyst. Macrocycles provided herein have a variety of uses in the pharmaceutical, biomedical, organic synthesis and chemical industries, such as the production of crown ethers that are useful as metal complexing species.
专利号:US-6946533-B2 优先权日:2002-08-01 标 题 :Synthesis of macrocyclic polymers by ring insertion polymerization of cyclic olefin monomers 发明人:GRUBBS ROBERT; BIELAWSKI CHRIS; BENITEZ DIEGO 权利人:CALIFORNIA INST OF TECHN 摘要:A method for synthesizing cyclic polymers using transition metal alkylidene complexes as reaction catalysts is provided, wherein the complexes contain a cyclic group. Polymerization is carried out on the catalyst, using cyclic olefin monomers that undergo ring insertion polymerization, and no linear intermediates are generated. Following completion of polymerization, the cyclic polymer detaches from the complex via an intramolecular chain transfer reaction and the catalytic complex is regenerated. The invention also provides novel transition metal alkylidene complexes useful as catalysts in the aforementioned process, as well as novel cyclic hydrocarbons.
专利号:US-8129521-B2 优先权日:2005-12-14 标 题 :One pot synthesis of tetrazole derivatives of rapamycin 发明人:DHAON MADHUP K; HSIAO CHI-NUNG; PATEL SUBHASH R; BONK PETER J; CHEMBURKAR SANJAY R; CHEN YONG Y 权利人:DHAON MADHUP K; HSIAO CHI-NUNG; PATEL SUBHASH R; BONK PETER J; CHEMBURKAR SANJAY R; CHEN YONG Y; ABBOTT LAB 摘要:A single-step, one-pot process to obtain zotarolimus and other rapamycin derivatives on large scale is presented, which improves currently available synthesis schemes. In one embodiment, dried rapamycin is dissolved in isopropylacetate (IPAc). The solution is cooled, and 2,6-Lutidine is added, followed slowly adding triflic anhydride at −30° C. Salts are then removed by filtration. Tetrazole, followed by a tert-base diisopropylethylamine (DIEA) is added to the triflate solution. After incubation at room temperature, the product is concentrated and purified by a silica gel column using THF/heptane as eluant. The fractions containing the product are collected, concentrated, and purified again using an acetone/heptane column. The product containing fractions are concentrated. The product is dissolved in t-BME and precipitated with heptane. The solids are dissolved in acetone, treated with butylated-hydroxy toluene (BHT), and the solution concentrated. The process is repeated twice with acetone to remove solvents. At least one stabilizing agent is added, such as BHT at 0.5% before drying.
专利号:WO-2015014261-A1 优先权日:2013-07-30 标 题:Macrolide compound or salt thereof, synthesis method, pharmaceutical composition, and application thereof 发明人:SHEN SHUNYI; CHEN DAIJIE; GE HAN; ZHANG ZHIHONG; REN YANSONG; LI ZHONGLEI; FAN QIANYONG; ZHANG YUN; XU YIJUN; LI DAN; LI JIAN 权利人:SHANGHAI INSITITUTE OF PHARMACEUTICAL INDUSTRY; CHINA STATE INST PHARM IND 摘要:The present invention discloses a macrolide compound or salt thereof, synthesis method, pharmaceutical composition, and application thereof. The present invention provides a method for preparing a macrolide compound 1, a macrolide compound 1', or a salt thereof; also provided are a macrolide compound 2, macrolide compound 2', or salt thereof, a pharmaceutical composition containing said compound or salt, and the application thereof in the preparation of a pharmaceutical for inhibiting methicillin-resistant Staphylococcus aureus. When one or more of the macrolide compound 2, the macrolide compound 2', the macrolide compound 2 salt, and the macrolide compound 2' salt of the present invention is used together with a β-lactam antibiotic, the inhibiting effect of the β-lactam antibiotic on methicillin-resistant Staphylococcus aureus is significantly increased. This is a new class of potentiator having a good potentiating effect in vitro, alleviating methicillin-resistant Staphylococcus aureus resistance to β-lactam antibiotics, and having good prospects for market development.
专利号:US-10669160-B2 优先权日:2018-04-30 标题:Heterogeneous wet synthesis process for preparation of high purity tungsten pentahalide 发明人:LIU YUMIN; LI FENG; WAN ZHIWEN; FAFARD CLAUDIA; WIESE STEFAN; HUSSON GUILLAUME; NIKIFOROV GRIGORY; SUI BIN; GIRARD JEAN-MARC 权利人:AIR LIQUIDE; AIR LIQUIDE AMERICAN 摘要:Synthesis of tungsten pentahalide compositions having low impurity profiles are disclosed. The specific impurity profile permits deposition of high purity tungsten-containing films using vapor deposition processes or other semiconductor manufacturing processes without introduction of performance-impacting contaminants.
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