专利号:US-5403937-A 优先权日:1993-04-30 标 题 :Process for preparing intermediates for the synthesis of antifungal agents 发明人:SAKSENA ANIL K; GIRIJAVALLABHAN VIYYOOR M; PIKE RUSSELL E; WANG HAIYAN; LOVEY RAYMOND G; LIU YI-TSUNG; GANGULY ASHIT K; MORGAN WILLIAM B; ZAKS ALEKSEY 权利人:SCHERING CORP 摘要:Disclosed is a process for preparing chiral compounds of the formula (I) (I) wherein: X1 and X2 are independently F or Cl; and E is -SO2R2, wherein R2 is C1-C6 alkyl, -C6H4CH3 or -CF3; its enantiomer and racemates thereof, useful in the synthesis of tetrahydrofuran azole antifungals. Novel compounds of the formula or wherein: X1 and X2 are independently F or Cl; B represents -C(O)Q* or -CH2OR''; Q* represents a chiral auxiliary group; R'' represents a hydroxy protecting group selected from -CH2C6H5, or -C(O)R1, wherein R1 is C1-C6 alkyl; and A represents Cl, Br, I or triazolyl; are also disclosed.
专利号:US-8778636-B2 优先权日:2009-05-22 标题:Chemo-enzymatic approach to the synthesis of pimecrolimus 发明人:GRISENTI PARIDE; REZA ELAHI SHAHRZAD; VERZA ELISA 权利人:GRISENTI PARIDE; REZA ELAHI SHAHRZAD; VERZA ELISA; EUTICALS SPA 摘要:Processes for preparing pimecrolimus starting from ascomycin, exploiting the selectivity characteristics of the purified enzymatic systems particularly regarding the selective functionalization of the hydroxyl groups present in position 24 and 33 of ascomycin. Such method represents the first example of chemoenzymatic synthesis for preparing pimecrolimus.
专利号:US-4950811-A 优先权日:1988-08-05 标题:Process for the preparation of trifluoro-ethanol by hydrolysis, in the gas phase, of chlorotrifluoroethane 发明人:DOUSSAIN CLAUDE; GUBELMANN MICHEL; TIREL PHILIPPE-JEAN 权利人:RHONE POULENC CHIMIE 摘要:A process for the preparation of trifluoroethanol by hydrolysis, in the gas phase, of chlorotrifluoroethane. A gaseous mixture of 1-chloro-2,2,2-trifluoroethane and water is contacted with a solid catalyst and taken to a temperature greater than 350 DEG C. and preferably between 400 DEG and 500 DEG C. 2,2,2-Trifluoroethanol (TFE) is a trifluorinated alcohol possessing very good thermal stability, which makes it suitable for a certain number of applications, in particular in the synthesis of fluorinated anesthetics, in pharmacology in general, and as a solvent.
专利号:US-5766887-A 优先权日:1996-08-26 标题 :Synthesis of 9-0-acetyl N-acetylneuraminic acid oligosaccharides 发明人:WONG CHI-HUEY; TAKAYAMA SHUICHI 权利人:SCRIPPS RESEARCH INST 摘要:Regioselective acetylation of the 9-hydroxyl group on N-acetylneuraminic acid is achieved enzymatically for producing oligosaccharides which contain a terminal N-acetylneuraminic acid moiety. This method provides access to O-acylated disialogangliosides as well as other N-acetyl-neuraminic acid oligosaccharides. These compounds are biologically and medicinally important and are difficult to obtain from nature or by chemical acylations. The methodology affords simple reaction conditions and minimal purification steps. In addition, the process affords good yields and the enzymes and reagents employed are commercially available with high stability and low costs.
专利号:WO-2023222057-A1 优先权日:2022-05-19 标 题 :Method for preparing self-assembling peptide rada16 by means of solid phase convergent synthesis 发明人:CHEN HONGYU; CHEN JINGSHUN; BI YAPING; LU JINGJING 权利人:JIANGSU AOSAIKANG PHARM CO LTD; NANJING HAIRUN PHARMACEUTICAL CO LTD 摘要:The present invention relates to the field of polypeptide synthesis, and provides a method for preparing a self-assembling peptide RADA16 by means of solid phase convergent synthesis. According to the present invention, a peptide fragment and a peptide resin are prepared by means of a solid-phase synthesis method, and the peptide fragment and the peptide resin are coupled to obtain a self-assembling peptide RADA16. According to the present invention, the purity of the prepared RADA16 crude product can reach 80% or more, and the method reduces the difficulty of separation and purification, is easy to operate, and uses readily available raw materials.
专利号:US-9359366-B2 优先权日:2013-04-10 标 题 :Intermediate of Ticagrelor and preparation method therefor, and preparation method for Ticagrelor 发明人:SUN SHAOGUANG; SONG DEFU; HE BIAO; LAI XIAOBO 权利人:JIANGSU HENGRUI MEDICINE CO; SUNCADIA PHARMACEUTICALS CO LTD 摘要:Disclosed are intermediates of Ticagrelor and a preparation method therefor, and a preparation method for Ticagrelor. Specifically, disclosed is an intermediate, namely, a compound of Formula (VI), for preparing Ticagrelor. Further disclosed is a method for preparing the intermediate and a method for preparing Ticagrelor by using the intermediate. Ticagrelor is prepared by using the intermediate, so that the synthesis process is simple, and a defect that long reaction times under high temperature that are required in the existing methods are avoided. The method is suitable for mass production in industry, energy consumption is reduced, pollution of the environment is reduced, and discharge of waste is reduced.
参考标题:Synthesis Of Nicotine Derivatives Via Reductive Disilylation Of (S)-Nicotine 作者:Emilie D. Smith,Florence C. Février,Daniel L. Comins |发布日期:2006.1.1 摘要:Variety Of Novel Nicotine Derivatives Were Prepared Via Reductive Disilylation Of (S)-Nicotine. Treatment Of Nicotine With Lithium Powder And Chlorotrimethylsilane Afforded 1,4-Bis(Trimethylsilyl)-1,4-Dihydronicotine In High Yield. Addition Of Various Carbonyl Electrophiles And A Catalytic Amount Of Tbaf Provided Either C-5 Substituted Nicotines Or 1,4-Dihydronicotine Derivatives.
合成参考文献
摘要:Schmidberger, J. W.; Hepworth, L. J.; Green, A. P.; Flitsch, S. L., Science of Synthesis: Biocatalysis in Organic Synthesis, (2015) 1, 344.