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:US-11186678-B2 优先权日:2018-11-30 标 题 :Radical cascade-enabled synthesis of precision polymers with complex main-chain structures 发明人:NIU JIA; HUANG HANCHU; WANG WENQI 权利人:TRUSTEES BOSTON COLLEGE 摘要:Radical cascade reactions enabling sequence-controlled ring-closing polymerization and ring-opening polymerization for the controlled synthesis of polymers with complex main-chain structures are provided. Facile syntheses leading to low-strain macrocyclic monomers consisting of the ring-opening triggers and extended main-chain structures are also provided. The present disclosure further provides methods for excellent control over polymer molecular weights and molecular weight distributions and high chain-end fidelity allows for the preparation of polymeric systems with well-defined architectures. Further provided are the general nature of the radical cascade-triggered transformations in polymer chemistry, and its application to the synthesis of polymers with diverse main-chain structural motifs with tailored functions. 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: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-2024083829-A1 优先权日:2020-12-31 标 题:Process for the asymmetric synthesis of isopiperitenol 发明人:LIST BENJAMIN; GRIMM JOYCE; ZHOU HUI; LIU LUPING; ZWERSCHKE ALEXANDER 权利人:STUDIENGESELLSCHAFT KOHLE GGMBH 摘要:The present invention refers to a process for the asymmetric synthesis of isopiperitenol and successor compounds.
专利号:US-9273023-B2 优先权日:2011-11-01 标 题:Modular synthesis of graphene nanoribbons and graphene substructures from oligo-alkynes 发明人:ALABUGIN IGOR; BYERS PHILIP M 权利人:UNIV FLORIDA STATE RES FOUND 摘要:A method for the synthesis of carbon-based structures, particularly graphene substructures and ribbons, from oligo- and poly-alkyne starting materials.
专利号:US-2004101523-A1 优先权日:1989-07-27 标题:Renal-selective prodrugs for control of renal smpathetic nerve activity in the treatment of hypertension 发明人:REITZ DAVID B; KOEPKE JOHN P; BLAINE EDWARD H; SCHUH JOSEPH R; MANNING ROBERT E; SMITS GLENN J 权利人:SEARLE & CO 摘要:Renal-selective prodrugs are described which are preferentially converted in the kidney to compounds capable of inhibiting synthesis of catecholamine-type neurotransmitters involved in renal sympathetic nerve activity. The prodrugs described herein are derived from inhibitor compounds capable of inhibiting one or more of the enzymes involved in catecholamine synthesis, such compounds being classifiable as tyrosine hydroxylase inhibitors, or as dopa-decarboxylase inhibitors, or as dopamine-β-hydroxylase inhibitors. These inhibitor compounds are linked to a chemical moiety, such as a glutamic acid derivative, by a cleavable bond which is recognized selectively by enzymes located predominantly in the kidney. The liberated inhibitor compound is then available in the kidney to inhibit one or more of the enzymes involved in catecholamine synthesis. Inhibition of renal catecholamine synthesis can suppress heightened renal nerve activity associated with sodium-retention related disorders such as hypertension. Conjugates of particular interest are glutamyl derivatives of dopamine-β-hydroxylase inhibitors, of which N-acetyl-γ-glutamyl fusaric acid hydrazide (shown below) is preferred.
参考文献:10.1002/marc.200900804 摘要:Biniek L, Chochos CL, Hadziioannou G, Leclerc N, Lévêque P, Heiser T. Electronic Properties and Photovoltaic Performances of a Series of Oligothiophene Copolymers Incorporating Both Thieno[3,2-b]thiophene and 2,1,3-Benzothiadiazole Moieties. Macromol Rapid Commun. 2010 Apr 06;31(7):651–6. doi: 10.1002/marc.200900804. 参考文献:10.1002/adma.201100297 摘要:Chen L, Li P, Cheng Y, Xie Z, Wang L, Jing X, Wang F. White electroluminescence from star-like single polymer systems: 2,1,3-benzothiadiazole derivatives dopant as orange cores and polyfluorene host as six blue arms. Adv Mater. 2011 Jul 12;23(26):2986–90. doi: 10.1002/adma.201100297.