专利号:WO-2022123336-A1 优先权日:2020-12-07 标 题 :Chromeno [4,3-b] quinoline compounds and their synthesis by using silicotungstic acid [h4siw12o40] 发明人:HEGDE SUBRAMANYA GOPAL; LOKESH KOODLUR SANNEGOWDA; SHUBHA JAYACHAMARAJAPURA PRANESH; SUSHMA NURANI VISWANATHAN; BASAVARAJU GIRISH; DANAGOUDAR ANANDA; BODA VIJAY KUMAR 权利人:HEGDE SUBRAMANYA GOPAL; LOKESH KOODLUR SANNEGOWDA 摘要:The present invention relates to the development of novel compounds of chromeno [4,3-b] quinolone derivatives. It particularly relates to the development of novel compounds of thiochromeno [4,3-b] quinolone derivatives for the treatment of coronary artery diseases, dyslipidemia, and metabolic syndrome. The present invention also relates to the first synthesis of Silicotungstic -catalyzed Aza-Diels-Alder-reactions (ADAR) with s-prenyl derivatives of α-tetralone, 4-chromanone and Thiochroman-4-one and various substituted amines to deliver cycloadducts in good yield and excellent diastereoselectivity under mild reaction conditions. The invention further relates to the method for the treatment of coronary artery diseases, dyslipidemia, and metabolic syndrome by using synthesized compounds of thiochromeno [4,3-b] quinolone derivatives. The present invention provides the use of Silicotungstic acid as Lewis acid for Aza-Diels-Alder-reactions to get a mixture of diastereomers are the first examples. In addition to its efficiency, simplicity, and mild reaction conditions, the catalyst is very cheap and only a small amount (10 mol%) is needed. Intramolecular cyclization was carried out very conveniently as a one-pot reaction starting from the S-prenyl chromene-3-carbaldehyde and arylamines without isolation of the intermediate imines.
专利号:EP-0818445-A1 优先权日:1996-07-09 标 题 :Preparation of intermediates useful in the synthesis of quinoline antibiotics 发明人:HAWKINS JOEL MICHAEL 权利人:PFIZER 摘要:A process for preparing a compound of the formulan nwherein R 1 , m, o and p are described below, which comprises adding a base of thenformulan nwherein R 2 , R 3 and R 4 are as described below, to a solution comprising a compoundnof the formula n nwherein R 1 , m, o and p are as described below, and a halonitromethane of the formulanO 2 NCH 2 X, wherein X is a halogen atom dissolved in a non-aqueous inert solvent.nThe compounds of formula III are useful as intermediates in the syntheses of azabicyclonquinoline carboxylic acids, and their pharmaceutically acceptable salts and prodrugs,nhaving antibacterial activity. This invention also relates to the base of formula IVnwherein each R 2 is butyl, R 3 is hydrogen and each R 4 is t -butyl.
专利号:WO-2015131100-A1 优先权日:2014-02-28 标题:Ligand-controlled c(sp3)-h arylation and olefination in synthesis of unnatural chiral alpha amino acids 发明人:YU JIN-QUAN 权利人:SCRIPPS RESEARCH INST 摘要:The use of ligands to tune the reactivity and selectivity of transition metal-catalysts for C(-sp3)-H bond functionalization is a central challenge in synthetic organic chemistry. Herein, we report a rare example of catalyst-controlled C(sp3)-H arylation using pyridine and quinoline derivatives: the former promotes exclusive monoarylation, whereas the latter activates the catalyst further to achieve diarylation. Successive application of these ligands enables the sequential diarylation of a methyl group in an alanine derivative with two different aryl iodides, affording a wide range of β-Ar-p-Ar ' -cc-amino acids with excellent levels of diastereoselectivity (d.r. > 20:1). Both configurations of the β-chiral center can be accessed by choosing the order in which the aryl groups are installed. The use of a quinoline derivative as a ligand also enables C(sp3)-H olefination of a protected alanine.
专利号:US-6072062-A 优先权日:1991-07-05 标 题 :Synthesis of C18 -modified vitamin D compounds and compounds resulting therefrom 发明人:VALLES MARIA J; MASCARENAS JOSEL; MOURINO ANTONIO; HALKES SEBASTIANUS J; ZORGDRAGER JAN 权利人:DUPHAR INT RES 摘要:The invention relates to a new vitamin D compound, substituted in the 18-position with an alkyl group, a hydroxy group, an alkoxy group, an alkenyl group, an alkynyl group, a fluorinated alkyl group or a fluorinated alkenyl group. The invention also relates to a method of preparing said vitamin D compound and to a lactone and a hydrindane intermediate. The vitamin D compound is of the general formula ##STR1##
专利号:EP-1189855-B1 优先权日:1999-07-02 标 题:Use of nitriles as polar aprotic solvents 发明人:LAURAIN NATHALIE; ZARD SAMIR 权利人:RHODIA CHIMIE SA 摘要:The invention concerns the use of aliphatic nitriles with relatively high molecular weight, as polar aprotic solvents, in particular in nucleophilic substitution reactions of the aromatic type. Said nitriles have a molecular mass more 79, preferably more than 90. The invention is useful for synthesis of fluorinated aromatic compounds.
专利号:EP-1756029-B1 优先权日:2004-04-08 标 题:Novel compounds, the preparation and the use thereof for a regiospesific synthesis of perfluor(alkyl) group heterocycles 发明人:EL KHARRAT SALEM; LAURENT PHILIPPE; BLANCOU HUBERT 权利人:CENTRE NAT RECH SCIENT; UNIV MONTPELLIER II 摘要:The invention relates to compounds of formula (1), wherein Z is a hydrogen or halogen atom; R'F is a perfluoroalkyl group CnF2n+1 in which n is an integer ranging from 1 to 12; R is in an ortho, meta or para position and represents an electron donor group, an electron attracting group, an aryl group or a heteroaryl group with the provision that R is an aryl or a heteroaryl. A method for preparing the inventive compounds (1) and a method for preparing heterocyclic compounds therefrom are also disclosed.
1: Jayaram V, Sridhar T, Sharma GVM, Berrée F, Carboni B. Synthesis of Polysubstituted Isoquinolines and Related Fused Pyridines from Alkenyl Boronic Esters via a Copper-Catalyzed Azidation/Aza-Wittig Condensation Sequence. J Org Chem. 2018 Jan 19;83(2):843-853. doi: 10.1021/acs.joc.7b02831. Epub 2018 Jan 5. 18(3):2001-2014. doi: 10.3892/etm.2019.7817. Epub 2019 Jul 26. 3: McPartland JM. Travell trigger points--molecular and osteopathic perspectives. J Am Osteopath Assoc. 2004 Jun;104(6):244-9. 50(3):367-9. doi: 10.1097/00007611-195703000-00015. sensitization to quotane and to para-aminobenzoic acid derivatives; report of a case with cross-sensitization reactions. N Y State J Med. 1953 Feb 15;53(4):442-4. English, Undetermined Language. 20(19):5617-24. doi: 10.1021/bi00522a041. 299(3):1038-48. 23(18):4023-33. doi: 10.1021/bi00313a003. 18(24):5464-75. doi: 10.1021/bi00591a032. 1054(2):213-8. doi: 10.1016/0167-4889(90)90243-7.
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摘要:S72 | NTUPHTW | Pharmaceutically Active Substances from National Taiwan University | DOI:10.5281/zenodo.3955664