专利号:US-11926589-B2 优先权日:2019-07-09 标 题 :Process for the synthesis of non-racemic cyclohexenes 发明人:REISMAN SARAH; ROMBOLA MICHAEL; LADD CAROLYN L; MCLAUGHLIN MARTIN JOHN; ZUEND STEPHAN; GOETZ ROLAND 权利人:BASF CORP; CALIFORNIA INST OF TECHN 摘要:This invention relates to a process for the synthesis of a non-racemic cyclohexene compound of formula (I) by a Diels-Alder reaction of a compound of formula (II) with a compound of formula (III) wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 , R 9 and Y have the meanings as defined in the description in the presence of a catalyst comprising at least one m-valent metal cation M m+ wherein the metal M is selected from Scandium (Sc), Yttrium (Y), Lanthanum (La), Cerium (Ce), Praseodymium (Pr), Neodymium (Nd), Promethium (Pm), Samarium (Sm), Europium (Eu), Gadolinium 15 (Gd), Terbium (Tb), Dysprosium (Dy), Holmium (Ho), Erbium (Er), Thulium (Tm), Ytterbium (Yb), Lutetium (Lu), Gallium (Ga) and Indium (In), and m is an integer of 1, 2 or 3, and a chiral ligand of the formula (IV) wherein R 10a , R 10b , R 10c , R 10d , R 10a′ , R 10b′ , R 10c′ , R 10d′ , Z and Z′ have the meanings as defined in the description.
专利号:WO-2024185734-A1 优先权日:2023-03-03 标 题:Polyphosphorylated nucleoside, phosphate-activated nucleotide used for synthesis of polyphosphorylated nucleoside and method for synthesis of same, and method for synthesis of polyphosphorylated nucleoside using phosphate-activated nucleotide 发明人:KATAOKA MASANORI; FUKUI CHIHARU; TSUJI YOHEI; FUJIMURA Kazuma 权利人:NATIAS INC 摘要:The present invention provides: a polyphosphorylated nucleoside which has a structure represented by formula (I) and can be efficiently produced by a short process and a simple operation with use of a less expensive material; a phosphate-activated nucleotide which is used for the synthesis of the polyphosphorylated nucleoside and a method for the synthesis of this phosphate-activated nucleotide; and a method for the synthesis of a polyphosphorylated nucleoside using a phosphate-activated nucleotide. In the formula, B represents a protected or unprotected, natural or artificial nucleoside base; R 1 , R 2 , R 4 and R 5 each represent H or an alkyl group or the like, and R 1 , R 2 , R 4 and R 5 may be the same as or different from each other; X and Y each represents H, OH, OCH 3 or the like; h represents an integer of 1 to 3; p, n, m and q each represent 0 or an integer, and p, n, m and q are in no particular order; and (p + n + m + q) is an integer of 0 to 5,000.
专利号:WO-0142264-A1 优先权日:1999-12-10 标 题 :Method for the synthesis of sialylated oligosaccharide donors 发明人:MEHTA SEEMA; GILBERT MICHEL; WAKARCHUK WARREN W; WHITFIELD DENNIS M 权利人:CA NAT RESEARCH COUNCIL; MEHTA SEEMA; GILBERT MICHEL; WAKARCHUK WARREN W; WHITFIELD DENNIS M 摘要:A method for the synthesis of aryl thioglycosides comprising a sialylated residue of β-D-galactose is disclosed. The method consists of preparing by a chemical synthesis a non-sialylated aryl thioglycoside, and enzymatically sialylating the latter with a sialic acid in the presence of a suitable sialyltransferase. The sialylated aryl thioglycoside is then chemically derivatized by standard procedures, to provide a derivative suitable for use as a donor in chemical syntheses of sialylated oligosaccharides. The derivatized sialylated aryl thioglycosides are prepared in high yields, due to reduced number of chemical and purification steps involved in the process. Derivatized aryl thioglycosides useful as building blocks for the synthesis of biologically active sialylated oligosaccharides are also disclosed.
专利号:US-2024116890-A1 优先权日:2022-09-28 标 题 :Large scale synthesis of cannabinol 发明人:COLLINS ARIANNA C; CRUCES IVAN; RAY KYLE; CRUCES WESTLEY 权利人:COLORADO CHROMATOGRAPY LLC 摘要:Methods for producing cannabinol, cannabivarin, or derivatives thereof are disclosed. The methods disclosed herein can be employed for large scale synthesis or semi-synthesis of the compounds, including multi-kilogram quantities of the compounds.
专利号:US-2022219156-A1 优先权日:2019-04-29 标题:Catalyst for the catalytic synthesis of urea 发明人:GLOTZBACH CHRISTOPH; TENHUMBERG NILS; EL HAWARY TAREK; MAKHYNYA YEVGENY; LEITNER WALTER; KLANKERMAYER JÜRGEN; SCHUMACHER HANNAH 权利人:THYSSENKRUPP IND SOLUTIONS AG; THYSSENKRUPP AG 摘要:A ruthenium-phosphine complex can be used as a catalyst in a method for the catalytic synthesis of urea. The method may comprise more particularly a reaction of formamide or of formamide with ammonia in the presence of the catalyst to form urea and hydrogen. Through the use of the ruthenium-phosphine complex as the catalyst, catalytic preparation of urea from formamide or from formamide with ammonia is provided for the first time. This allows for synthesis under mild conditions and virtually no formation of byproducts. Further, using an acid as a cocatalyst in the catalytic synthesis or the reaction can lead to an improvement in urea yield.
专利号:US-11912647-B2 优先权日:2020-05-22 标 题:Diversity-oriented synthesis of N,N,O-trisubstituted hydroxylamines from alcohols and amines by N—O bond formation 发明人:CRICH DAVID; HETTIKANKANAMALAGE ASIRI; HILL JARVIS 权利人:UNIV GEORGIA 摘要:In one aspect, the disclosure relates to a method for the direct synthesis of complex N,N,O-trisubstituted hydroxylamines by N—O bond formation. In another aspect, the method can successfully be employed using a wide variety of commercially available alcohols and secondary amines and enables the construction of large fragment-based libraries of trisubstituted hydroxylamines for drug discovery purposes. Also disclosed are N,N,O-trisubstituted hydroxylamines having low basicity, high stability at ambient temperatures, and an inherent lack of reactivity towards acetylating and sulfonylating enzymes that confer mutagenicity on less-substituted hydroxylamines.
参考文献:10.1021/jo201514q 摘要:Yang F, Ji K, Ali S, Liang Y. Sc(OTf)3-Catalyzed Synthesis of Indoles and SnCl4-Mediated Regioselective Hydrochlorination of 5-(Arylamino)pent-3-yn-2-ones. J. Org. Chem. 2011 Sep 16;76(20):8329–35. doi: 10.1021/jo201514q. 参考文献:10.1021/ol400371h 摘要:Li X, Wang H, Yang S. Sc(OTf)3-Catalyzed Dehydrogenative Cyclization for Synthesis of N-Methylacridones. Org. Lett. 2013 Mar 29;15(8):1794–7. doi: 10.1021/ol400371h. 参考文献:10.1021/acs.joc.1c01912 摘要:Gou BB, Yang S, Sun HR, Jian QS, Sharif A, Zhou L, Chen J. Scandium Triflate Catalyzed Tandem Transfer Hydrogenation and Cyclization Reaction of o-Aminobenzaldehydes and o-Aminoacetophenone with Alcohols. J Org Chem. 2021 Dec 17;86(24):17673–83. doi: 10.1021/acs.joc.1c01912.