专利号:US-11161827-B2 优先权日:2019-04-05 标 题 :Catalytic systems for stereoselective synthesis of chiral amines by enantiodivergent radical C—H amination 发明人:Zhang xiao-xiang; Lang kai 权利人:TRUSTEES BOSTON COLLEGE; THE TRUSTEES OF BOSTON COLLEGE 摘要:In one aspect, the disclosure relates to a mode of asymmetric induction in radical processes based on sequential combination of enantiodifferentiative H-atom abstraction and stereoretentive radical substitution. Also disclosed is an asymmetric system for stereoselective synthesis of strained 5-membered cyclic sulfamides via radical 1,5-C—H amination of sulfamoyl azides. The disclosed metalloradical system can control the degree and sense of asymmetric induction in the catalytic radical C—H amination in a systematic manner. The disclosed system is applicable to a broad scope of substrates with different types of C(sp 3 )—H bonds and exhibits reactivity and selectivity, providing access to both enantiomers of useful 5-membered cyclic sulfamides in a highly enantioenriched form. Also disclosed are catalysts useful in these processes. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present disclosure.
专利号:WO-2024036115-A1 优先权日:2022-08-08 标题:Continuous flow synthesis of lorazepam 发明人:THOMPSON DAVID; BIYANI SHRUTI; HYUN SEOK-HEE; MCGUIRE MICHAEL 权利人:PURDUE RESEARCH FOUNDATION; CONTINUITY PHARMA LLC 摘要:A method for synthesis of Lorazepam in a continuous flow using continuous flow reactor, in which method comprises five steps including N-acylation, diazepine ring closure, imine N- oxidation, Polonovski-type rearrangement, and ester hydrolysis; a green reagent comprising a peroxide reagent and rhenium oxide catalyst for N-oxidation of delorazepam; and an ammonium source combination for the synthesis of delorazepam.
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.
专利号:US-2024368099-A1 优先权日:2022-01-18 标 题:Methods for the synthesis of di(hydroxymethyl)tetrahydrofuran and its application in polyesters and polyurethanes 发明人:SPIEGELBERG BRIAN; BRANDT ADRIAN; BECK HORST; KUX ALEXANDER; TIN SERGEY; DE VRIES JOHANNES GERARDUS 权利人:HENKEL AG & CO KGAA 摘要:The present invention relates to the synthesis of di(hydroxymethyl)tetrahydrofuran (DHMTHF) and the preparation of trans-enriched mixtures of DHMTHF. The invention further refers to polyester polyols which are obtained by reaction of cis/trans DHMTHF mixtures with a dicarboxylic acid. The invention further relates to polyurethanes and compositions containing a polyester polyol comprising DHMTHF, in particular to such polyurethane-containing (adhesive) compositions.
专利号:US-6399536-B2 优先权日:2000-02-11 标 题 :High performance catalyst systems for the synthesis of alkylenecarbonates 发明人:KIM HOON SIK; LEE BYUNG GWON; LEE SANG DEUK; KWON YOUNG SOO; LEE HYUN JOO 权利人:KOREA INST SCI & TECH 摘要:A catalyst of the formula (1) for the synthesis of alkylene carbonate by reacting alkylene oxide and carbon dioxide n n n L m MX n   (1) n n n wherein L is selected from a group of pyridines; n M is a metal atom selected from Zn, Fe, Mn, Pb and In; n X is a halogen atom selected from Cl, Br and I; n m is 1 or 2, and n n is 2 or 3.
专利号:WO-9900440-A1 优先权日:1997-06-26 标 题:Synthesis of a dendritic polyalcohol 发明人:IHRE HENRIK; HULT ANDERS 权利人:PERSTORP AB; IHRE HENRIK; HULT ANDERS 摘要:A process for a double stage convergent synthesis of a polymeric polyalcohol substantially and preferably built up from polyester units and composed of a monomeric or polymeric core to which at least one hyperbranched dendritic branch (dendron) consisting of a number of branching generations is added. The branching generations comprise a polymeric or monomeric branching chain extender having three reactive functions of which two are hydroxyl groups and one is a carboxyl group. The two hydroxyl groups of the branching chain extender is in a first step ketal protected by reacting said two hydroxyl groups with a ketal. A second step includes protection of the carboxyl group of said branching chain extender. The ketal protected branching chain extender and the carboxyl protected chain extender are then employed for repeated addition in a number of step yielding a predetermined number of branching generations. The thus synthesized dendron is finally added to a core having reactive hydroxyl or epoxide groups and the ketal protected hydroxyl groups are optionally deprotected.
摘要:Ogawa, C.; Kobayashi, S., Science of Synthesis: Water in Organic Synthesis, (2012) 1, 586. 摘要:Pineschi, M.; Boldrini, C., Science of Synthesis: Advances in Organoboron Chemistry towards Organic Synthesis, (2019) 1, 218. 摘要:Geetharani, K.; Bose, S. K., Science of Synthesis: Advances in Organoboron Chemistry towards Organic Synthesis, (2019) 1, 346. 摘要:Yerien, D. E.; Barata-Vallejo, S.; Postigo, A., Science of Synthesis: Modern Strategies in Organofluorine Chemistry , (2024) 1, 5.