专利号:US-11459549-B2 优先权日:2018-05-10 标 题:Method for biocatalytic synthesis of Sitagliptin and intermediate thereof 发明人:WU FAHAO; YANG WEN; LI GANG; SHI HONGWEI; GAO YANGZHE; LIU LILI; YUAN ZHIFA 权利人:CHINA FORTUNE WAY COMPANY; NANJING REDWOOD FINE CHEMICAL CO LTD 摘要:Provided is a method for biocatalytic synthesis of Sitagliptin and intermediates thereof, in particular, provided are compounds of Formula (I) and Formula (II), or pharmaceutically acceptable salts thereof, a polypeptide capable of catalyzing conversion of a compound of Formula (I) to a compound of Formula (II), a nucleic acid encoding the polypeptide, a vector and a cell comprising the nucleic acid. In addition, also provided are a method for producing a compound of Formula (II) and Sitagliptin by using the polypeptide and the compound of Formula (I), and a method for preparing the polypeptide.
专利号:US-8889921-B2 优先权日:2010-10-13 标题:Methods of synthesis of scyllitol and related compounds 发明人:GREENFIELD SCOTT 权利人:GREENFIELD SCOTT; TRANSITION THERAPEUTICS IRELAND LTD 摘要:Methods of synthesis of scyllitol diborate and related compounds are provided, including methods that are performed in all-aqueous solutions. Also provided are methods in which the reaction products are recycled to increase the efficiency of the process. The methods include the steps of conversion of a solution of inositol to scyllitol, conversion of scyllitol in the solution to scyllitol diborate, and isolation of the scyllitol diborate from the solution. The scyllitol diborate is reacted to form substantially pure scyllitol diborate, and the remaining solution is efficiently recycled to scyllitol diborate, then to additional substantially pure scyllitol. This scyllitol diborate recycling step can be applied to a variety of processes to improve the yield of scyllitol. The methods are highly efficient and result in large scale reaction products of high purity.
专利号:US-3983145-A 优先权日:1973-11-01 标 题:Use of alpha-di(lower alkoxy) anthraquinones in the synthesis of Alizarin Saphirols 发明人:WHITE DAVID L; FITZPATRICK JOSEPH W 权利人:TOMS RIVER CHEMICAL CORP 摘要:Alpha-dihydroxyanthraquinones used as intermediates in the synthesis of many dyestuffs, such as the Alizarin Saphirols (e.g. Color Constitution No. 63000, 63005, 63010, 63011, 63315 and 63610) can be replaced on an equimolar basis by alpha-di(lower alkoxy)anthraquinones. The alpha-di(lower alkoxy) anthraquinones can be converted in a single step, by treatment with oleum, to the corresponding alpha-dihydroxyanthraquinone-beta-disulfonic acids in almost quantitative yield. The corresponding diamine is obtained by dinitrating followed by reduction of the nitro groups. The known intermediate, leuco 1,4,5,8-tetrahydroxyanthraquinone (see C.I. No. 62500) can be obtained either by reduction of the diamine or by reduction of the dinitro compound. In one embodiment, the alpha-di(lower alkoxy)anthraquinone is obtained from dinitroanthraquinone by treatment thereof with methanol and KOH.
专利号:US-4003916-A 优先权日:1975-12-22 标 题:Total synthesis of steganacin and derivatives thereof 发明人:KENDE ANDREW S; LIEBESKIND LANNY S 权利人:KENDE ANDREW S; LIEBESKIND LANNY S 摘要:Steganacin and Steganangin, dibenzocyclooctadiene lignan lactones, have been reported to possess antileukemic activity. This invention describes the first total synthesis of these compounds and other relevant intermediates.
专利号:US-4059593-A 优先权日:1975-12-22 标 题:Synthesis of steganacin and derivatives thereof 发明人:KENDE ANDREW S; LIEBESKIND LANNY S 权利人:UNIV ROCHESTER 摘要:Steganacin and Steganangin, dibenzocyclooctadiene lignan lactones, have been reported to possess anti-leukemic activity. This invention describes the first total synthesis of these compounds and other relevant intermediates.
专利号:US-9982005-B2 优先权日:2013-04-04 标 题 :Macrolides and methods of their preparation and use 发明人:MYERS ANDREW G; SEIPLE IAN BASS; ZHANG ZIYANG 权利人:HARVARD COLLEGE 摘要:Provided herein are methods of preparing macrolides by the coupling of an eastern and western half, followed by macrocyclization, to provide macrolides, including both known and novel macrolides. Intermediates in the synthesis of macrolides including the eastern and western halves are also provided. Pharmaceutical compositions and methods of treating infectious diseases and inflammatory conditions using the inventive macrolides are also provided. A general diastereoselective aldol methodology used in the synthesis of the western half is further provided.
参考文献:10.1007/s00216-016-9671-0 摘要:Diserens G, Vermathen M, Gjuroski I, Eggimann S, Precht C, Boesch C, Vermathen P. Direct determination of phosphate sugars in biological material by 1H high-resolution magic-angle-spinning NMR spectroscopy. Analytical and Bioanalytical Chemistry. 2016 Jun 06;408(20):5651–6. doi: 10.1007/s00216-016-9671-0.