38025-45-5Relevant academic research and scientific papers
Synthetic method of 4 -phenyl piperidine hydrochloride
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Paragraph 0011; 0052; 0054; 0057; 0059; 0062; 0064; ..., (2021/11/06)
The invention discloses a synthesis method of 4 -phenylpiperidine hydrochloride, and the route is as shown in the specification. The method has the advantages of cheap and easily available raw materials, simple operation and post-treatment, high yield, high product purity and the like, and is suitable for industrial production.
Transition-Metal-Free Deconstructive Lactamization of Piperidines
Romero-Iba?ez, Julio,Cruz-Gregorio, Silvano,Sandoval-Lira, Jacinto,Hernández-Pérez, Julio M.,Quintero, Leticia,Sartillo-Piscil, Fernando
supporting information, p. 8867 - 8871 (2019/05/28)
One of the major challenges in organic synthesis is the activation or deconstructive functionalization of unreactive C(sp3)–C(sp3) bonds, which requires using transition or precious metal catalysts. We present here an alternative: the deconstructive lactamization of piperidines without using transition metal catalysts. To this end, we use 3-alkoxyamino-2-piperidones, which were prepared from piperidines through a dual C(sp3)–H oxidation, as transitory intermediates. Experimental and theoretical studies confirm that this unprecedented lactamization occurs in a tandem manner involving an oxidative deamination of 3-alkoxyamino-2-piperidones to 3-keto-2-piperidones, followed by a regioselective Baeyer–Villiger oxidation to give N-carboxyanhydride intermediates, which finally undergo a spontaneous and concerted decarboxylative intramolecular translactamization.
CEREBLON BINDERS FOR THE DEGRADATION OF IKAROS
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Page/Page column 332; 333, (2019/10/23)
The present invention provides cereblon binders for the degradation of Ikaros or Aiolos by the ubiquitin proteasome pathway along with their use in therapeutic applications as described herein.
Efficient and chemoselective reduction of pyridines to tetrahydropyridines and piperidines via rhodium-catalyzed transfer hydrogenation
Wu, Jianjun,Tang, Weijun,Pettman, Alan,Xiao, Jianliang
, p. 35 - 40 (2013/03/13)
Promoted by iodide anion the rhodium complex dimer, [Cp RhCl 2]2, catalyzes efficiently the transfer hydrogenation of various quaternary pyridinium salts under mild conditions, affording not only piperidines but also 1,2,3,6-tetrahydropyridines in a highly chemoselective fashion, depending on the substitution pattern at the pyridinium ring. The reduction is conducted in azeotropic formic acid/triethylamine (HCOOH-Et 3N) mixture at 40 °C, with catalyst loadings as low as 0.005mol% being feasible. Copyright
Synthesis and SAR study of 4-arylpiperidines and 4-aryl-1,2,3,6- tetrahydropyridines as 5-HT2C agonists
Conway, Richard J.,Valant, Celine,Christopoulos, Arthur,Robertson, Alan D.,Capuano, Ben,Crosby, Ian T.
supporting information; experimental part, p. 2560 - 2564 (2012/05/05)
A series of substituted 4-arylpiperidines and a smaller family of 4-aryl-1,2,3,6-tetrahydropyridines were synthesized and their biological activity at the 5-HT2C receptor studied to determine whether either series showed noteworthy agonist activity. Structure-activity relationships were developed from the performed receptor binding assays and functional studies, and the results of the analysis are presented herein.
A strategy for isotope containment during radiosynthesis - Devolatilisation of bromobenzene by fluorous-tagging-Ir-catalysed borylation en route to the 4-phenylpiperidine pharmacophore
Spivey, Alan C.,Martin, Laetitia J.,Tseng, Chih-Chung,Ellames, George J.,Kohler, Andrew D.
supporting information; experimental part, p. 4093 - 4095 (2009/02/07)
Syntheses of two 4-phenylpiperidines from bromobenzene have been developed involving anchoring to a fluorous-tag, Ir-catalysed borylation, Pd- and Co-catalysed elaboration then traceless cleavage. Although performed using 'cold' (i.e. unlabelled) bromoben
SYNTHESIS OF UNSATURATED PIPERIDINES FROM PIPERIDONES WITH A SILYL REAGENT
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Page/Page column 20, (2008/12/07)
Syntheses of unsaturated piperidines from piperidones through a silyl pipehdine reagent via the Shapiro reaction and palladium-catalyzed cross- coupling reactions with organo halides.
Palladium(0)-catalyzed alkynyl and allenyl iminium ion cyclizations leading to 1,4-disubstituted 1,2,3,6-tetrahydropyridines
Tsukamoto, Hirokazu,Kondo, Yoshinori
supporting information; experimental part, p. 4851 - 4854 (2009/02/08)
(Chemical Equation Presented) The biologically important title heterocyclic compounds can be synthesized by two methods based on the cyclization of alkynyl and allenyl iminium ions generated in situ in the presence of organometallic reagents (see scheme).
Synthesis of 4-arylpiperidines from 1-benzyl-4-piperidone: Application of the shapiro reaction and alkenylsilane cross-coupling
Morrill, Christie,Mani, Neelakandha S.
, p. 1505 - 1508 (2008/02/02)
Equation Presented 1-Benzyl-3,4-unsaturated-4-piperidinyl benzyldimethylsilane has been prepared and observed to readily undergo palladium-catalyzed cross-coupling reactions with a variety of aryl iodides and aryl bromides to generate 3,4-unsaturated 4-arylpiperidines, often at ambient temperature.
PYRAZOLONE COMPOUNDS AS METABOTROPIC GLUTAMATE RECEPTOR AGONISTS FOR THE TREATMENT OF NEUROLOGICAL AND PSYCHIATRIC DISORDERS
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Page/Page column 129; 130, (2008/06/13)
Compounds of Formula (I), wherein R1, R2, R3, R4, R5, R6, X, and n are as defined for Formula (I) in the description, processes for the preparation of the compounds and new intermediates employed in the preparation, pharmaceutical compositions containing the compounds, and the use of the compounds in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction.
