乙烯基溴化镁置于硼酸三甲酯,Potassium Hydrogen Bifluoride体系中,用 四氢呋喃 用作溶剂,化学反应 0.83H,以71%的收率获得乙烯三氟硼酸钾 参考文献:One-Pot Formation Of Nitrogen-Containing Heterocyclic Ring Systems Using A Deprotection-cyclisation-asymmetric Reduction Sequence 标题:One-Pot Formation Of Nitrogen-Containing Heterocyclic Ring Systems Using A Deprotection-cyclisation-asymmetric Reduction Sequence 摘要:一种单锅反应的胺去保护,分子内cn键的形成以及随后不对称还原反应可能由一种钌催化剂促进. Doi:10.1039/b509231K
专利号:US-10793495-B2 优先权日:2015-08-14 标 题:Synthesis of polyaryl substituted aryl compounds 发明人:BOULOS RAMIZ; FEUTRILL JOHN 权利人:BOULOS & COOPER PHARMACEUTICALS PTY LTD 摘要:A method for the synthesis of a aryl compound of Formula (1).n nU T-W—R 1 ) n    (1)
专利号:US-2025304580-A1 优先权日:2021-11-09 标 题:Heterocyclic compounds as triggering receptor expressed on myeloid cells 2 agonists and methods of use 发明人:HOUZE JONATHAN B; PANDYA BHAUMIK; KAPLAN ALAN P; BOS MAXENCE; MANCUSO JOHN; FRANZONI IVAN 权利人:VIGIL NEUROSCIENCE INC 摘要:The present disclosure provides compounds of Formula I, useful for the activation of Triggering Receptor Expressed on Myeloid Cells 2 (“TREM2â€?).This disclosure also provides pharmaceutical compositions comprising the compounds, uses of the compounds, and compositions for treatment of, for example, a neurodegenerative disorder. Further, the disclosure provides intermediates useful in the synthesis of compounds of Formula I.
专利号:US-12319691-B2 优先权日:2020-05-04 标题 :Heterocyclic compounds as triggering receptor expressed on myeloid cells 2 agonists and methods of use 发明人:CZABANIUK LARA C; HOPPER TIMOTHY; HOUZE JONATHAN B; RESCOURIO GWENAELLA; SANTORA VINCENT; WANG HAOXUAN; WHITE RYAN D; WONG ALICE R; WU YONGWEI 权利人:AMGEN INC; VIGIL NEUROSCIENCE INC 摘要:The present disclosure provides compounds of Formula I, useful for the activation of Triggering Receptor Expressed on Myeloid Cells 2 (“TREM2â€?).This disclosure also provides pharmaceutical compositions comprising the compounds, uses of the compounds, and compositions for treatment of, for example, a neurodegenerative disorder. Further, the disclosure provides intermediates useful in the synthesis of compounds of Formula I.
专利号:EP-3747957-A1 优先权日:2019-06-07 标 题:Fluorescent vinyl tiophene and bitiophene coumarins dyes and method of synthesis thereof 发明人:PEREIRA ANTONIO; MARTINS SÉRGIO; CALDEIRA ANA; CANDEIAS ANTÓNIO; EUSTÃ?QUIO RAQUEL; SILVA SOFIA 权利人:UNIV EVORA 摘要:The present invention relates to fluorescent vinyl thiophene and bithiophene coumarins, in particular to 7-alkylamino-3-vinyl thiophene and 7-alkylamino-3-vinyl dithiophene coumarin compounds of general formula (I), their derivatives, method of synthesis and uses thereof as fluorescent dyes for tagging biomolecules and as dye-sensitized solar cells (DSSCs).n n Therefore, the present invention is in the technical domain of biochemistry, molecular biology and biology and is useful to be applied in research and diagnosis, including medical diagnosis.
专利号:WO-2012107532-A1 优先权日:2011-02-11 标 题 :4-aminoalcoholquinoline derivatives, enantioselective synthesis methods and the use thereof 发明人:JONET ALEXIA; DASSONVILLE-KLIMPT ALEXANDRA; MULLIE CATHERINE; TAUDON NICOLAS; SONNET PASCAL 权利人:UNIV PICARDIE; JONET ALEXIA; DASSONVILLE-KLIMPT ALEXANDRA; MULLIE CATHERINE; TAUDON NICOLAS; SONNET PASCAL 摘要:The present invention is intended to provide new antimalarial compounds with a strong antimalarial activity as well as antibacterial activity with few neurological side effects and a new enantioselective pathway to mefloquine amino-analogs allowing the access of such compounds. The present invention relates to new 4 -aminoalcohol quinoline derivatives of formula (I), as well as the synthesis methods and the uses of such derivatives. In which Y is one selected from formulae (II) to (III). In which Z is selected from formulae (IV) to (VI), and wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 and n are as defined in the claims.
专利号:WO-2023072966-A1 优先权日:2021-10-26 标题:Imidazolone derivatives as inhibitors of protein kinases in particular dyrk1a, clk1 and/or clk4 发明人:DEAU EMMANUEL; GEORGE PASCAL; MEIJER LAURENT; MIEGE FRÉDÉRIC 权利人:PERHA PHARMACEUTICALS 摘要:The present invention relates to a compound of formula (I) wherein R 1 represents a (C 4 -C 6) alkyl group, a (C 3 -C 8) cycloalkyl group, a bridged (C 6 -C 10 )cycloalkyl group, a fused phenyl group, a substituted phenyl group, a R'-L- group, wherein L is either a single bond or a (C 1 -C 3 )alkanediyl group, and R' represents, a (C 3 -C 8 )heterocycloalkyl group, or a (C 3 -C 8 )heteroaryl group, or a R''-L- group wherein L is a (C 1 -C 3 )alkanediyl group, and R'' is an optionally substituted phenyl group; R 2 is selected from the group consisting of a hydrogen atom and a (C 1 -C 3 )alkyl group; R 5 represents a hydrogen atom, a (C 1 -C 4 )alkyl group or a (C 3 -C 6 )cycloalkyl group or any of its pharmaceutically acceptable salt. The present invention further relates to a composition comprising a compound of formula (I) and a process for manufacturing said compound as well as its synthesis intermediates. It also relates to said compound for use as a medicament, in particular in the treatment and/or prevention of cognitive deficits and neuroinflammation associated with Down syndrome; Alzheimer's disease; dementia; tauopathies; Parkinson's disease; CDKL5 Deficiency Disorder; Phelan-McDermid syndrome; autism; type 1 and type 2 diabetes; abnormal folate and methionine metabolism; osteoarthritis and tendinopathy; Duchenne muscular dystrophy; cancers and leukemias; neuroinflammation, anemia, infections caused by unicellular parasites, viral infections and for regulating body temperature.