专利号:US-11713329-B2 优先权日:2018-12-10 标 题 :Intermediates useful in the preparation of halichondrin compounds and methods for preparing the same 发明人:XU WEIPING 权利人:BEIJING TIENYI LUFU PHARMATECH CO LTD 摘要:The invention relates to intermediates useful in the preparation of halichondrin compounds, methods for preparing the same and use thereof, such as halichondrins, eribulin, or their analogs. The intermediates, the methods and use thereof are used for the synthesis of the C20-C26 fragment of halichondrin compounds. The raw materials in the synthetic route of the invention are cheap and easily obtained, the sources and the qualities of the raw materials are reliable. The choice of the methods useful in the synthesis of chiral central structures are based on the structural characteristics of the reactants, thus effectively improving the synthesis efficiency, reducing the difficulties and risks of product quality control, and avoiding the use of highly toxic and expensive organotin catalysts to significantly decrease costs and improve environmental friendliness.
专利号:US-5162495-A 优先权日:1989-11-13 标 题:Synthesis of quinoline and substituted quinoline copolymers 发明人:CHIANG LONG Y; SWIRCZEWSKI JOHN W 权利人:EXXON RESEARCH ENGINEERING CO 摘要:The present invention is predicated on the discovery that quinoline and substituted quinoline derivatives, having substituents in positions other than the 2 and 6 position, undergo polymerization in the presence of tetrahydroquinoline or substituted tetrahydroquinolines and a transition metal sulfide catalyst to produce polymers that have repeating quinoline and substituted moieties. Thus, in one embodiment of the present invention, there is provided a novel method of preparing polymers having the formula (7) which comprises contacting a tetrahydroquinoline having the formula (8) with a quinoline compound having the formula (9) at elevated temperatures and in the presence of a transition metal sulfide catalyst wherein the metal is selected from Groups VIB, VIIB of the periodic table and mixtures thereof and wherein the Rs (i.e. R3, R4, etc.) and the R's (i.e. R'3, R'4, etc.) may be the same or different and are selected from hydrogen, halogen (especially fluoro-, chloro- and bromo-), -NO2, OH, -NH2, -SH, -CN and organic substituents. In the above polymer, x and y represent the relative proportion of bracketed structural quinoline or substituted moieties, and n is an integer equal to or greater than 2.
专利号:US-2011144326-A1 优先权日:2009-12-10 标题:Method for manufacturing stereoselective preparation of 4-BMA using a chiral auxiliary and chiral auxiliary 发明人:TSENG WEI-HONG; CHUANG SHIUAN-TING; HUNG ZUN-YUAN; WU CHING-I 权利人:TSENG WEI-HONG; CHUANG SHIUAN-TING; HUNG ZUN-YUAN; WU CHING-I 摘要:The present invention relates to a process for preparing (3R,4S)-3-[[[R]-1′-t-butyldimethylsilyloxy]ethyl]-4-[(R)-1″-carboxyethyl]-2-azetidinone (beta-methylazetidin-2-one; 4-BMA), a key intermediate for the synthesis of carbapenem and penem antibiotics. Specifically, the present invention relates to a process comprising first, the preparation of a chiral auxiliary from cheap L-Phenylalaninol, and then the preparation of 4-BMA in high yield and high selectivity, under industrially mild condition.
专利号:EP-2345645-A1 优先权日:2009-12-22 标题 :Method for manufacturing stereoselective preparation of 4-bma using a chiral auxiliary and chiral auxiliary 发明人:TSENG WEI-HONG; CHUANG SHIUAN-TING; HUNG ZUN-YUAN; WU CHING-I 权利人:SAVIOR LIFETEC CORP 摘要:The present invention relates to a process for preparing (3R,4S)-3- [[[R]-1 ' -t-butyldimethylsilyloxy ]ethyl]-4-[(R)-1 '-carboxyethyl]-2-azetidinone (beta- methylazetidin-2-one; 4-BMA), a key intermediate for the synthesis of carbapenem and penem antibiotics. Specifically, the present invention relates to a process comprising first, the preparation of a chiral auxiliary from cheap L-Phenylalaninol, and then the preparation of 4-BMA in high yield and high selectivity, under industrially mild condition.
专利号:US-3766236-A 优先权日:1970-11-27 标 题 :Synthesis of halothiolformates 发明人:THALER W; MUELLER W 权利人:EXXON RESEARCH ENGINEERING CO 摘要:HALOTHIOLFORMATES ARE PREPARED BY REACTING A SULFENYL HALIDE WITH CARBON MONOXIDE UNDER MODERATE CONDITIONS OF TEMPERATURE AND PRESSURE, THE PRODUCTS BEING USEFUL AS PESTICIDES AND AS INTERMEDIATES FOR THE PREPARATION OF CARBAMATE PESTICIDES; REACTIVITY OF THE SULFENYL HALIDE MAY BE ENHANCED BY HEAT, POLAR SOLVENTS, AND/OR LEWIS ACID CATALYSTS.
专利号:US-9079164-B2 优先权日:2012-03-26 标题:Single reaction synthesis of texturized catalysts 发明人:WOODFIELD BRIAN F; SMITH STACEY; SELCK DAVID; BARTHOLOMEW CALVIN H; MA XUCHU; XU FEN; OLSEN REBECCA E; ASTLE LYNN 权利人:UNIV BRIGHAM YOUNG 摘要:Methods are described for making a texturized catalyst. The textural promoter may be a high-surface area, high-porosity, stable metal oxide support. The catalyst is manufactured by reacting catalyst precursor materials and support materials in a single, solvent deficient reaction to form a catalyst. The catalyst may be particles or a coating or partial coating of a support surface.