79601-21-1Relevant academic research and scientific papers
TRIAZACYCLODODECANSULFONAMIDE ("TCD")-BASED PROTEIN SECRETION INHIBITORS
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Paragraph 00256, (2019/10/04)
Provided herein are triazacyclododecansulfonamide ("TCD")-based protein secretion inhibitors, such as inhibitors of Sec61, methods for their preparation, related pharmaceutical compositions, and methods for using the same. For example, provided herein are compounds of Formula (I) and pharmaceutically acceptable salts and compositions including the same. The compounds disclosed herein may be used, for example, in the treatment of diseases including inflammation and/or cancer.
Decarboxylative Negishi Coupling of Redox-Active Aliphatic Esters by Cobalt Catalysis
Liu, Xu-Ge,Zhou, Chu-Jun,Lin,Han, Xiang-Lei,Zhang, Shang-Shi,Li, Qingjiang,Wang, Honggen
supporting information, p. 13096 - 13100 (2018/09/21)
A cobalt-catalyzed decarboxylative Negishi coupling reaction of redox-active aliphatic esters with organozinc reagents was developed. The method enabled efficient alkyl–aryl, alkyl–alkenyl, and alkyl–alkynyl coupling reactions under mild reaction conditions with no external ligand or additive needed. The success of an in situ activation protocol and the facile synthesis of the drug molecule (±)-preclamol highlight the synthetic potential of this method. Mechanistic studies indicated that a radical mechanism is involved.
Cobalt-Catalyzed Cross-Coupling of 3- and 4-Iodopiperidines with Grignard Reagents
Gonnard, Laurine,Gurinot, Amandine,Cossy, Janine
supporting information, p. 12797 - 12803 (2015/09/01)
A cobalt-catalyzed cross-coupling between 3- and 4-iodopiperidines and Grignard reagents is disclosed. The reaction is an efficient, cheap, chemoselective, and flexible way to functionalize piperidines. This coupling was used as the key step to realize a short synthesis of (±)-preclamol. Some mechanistic investigations were conducted that highlight the formation of radical intermediates. Scaffold synthesis: A cobalt-catalyzed cross-coupling between iodopiperidines and Grignard reagents is reported (see scheme; PG=protecting group). A large variety of 3- and 4-substituted piperidines were synthesized and the method was applied to a short synthesis of (±)-preclamol. This work constitutes one of the rare examples of cross-couplings involving 3-halogeno piperidines.
Concise synthesis of 3-arylpiperidines
Chang, Meng-Yang,Hsu, Ru-Ting,Chen, Hua-Ping,Lin, Pei-Jung
, p. 1173 - 1183 (2007/10/03)
We present an easy and straightforward synthesis of 3-arylpiperidines by Grignard addition of piperidin-3-one with different arylmagnesium bromide reagents and acidic dehydroxylation of the resulting tertiary alcohol with the combination of triethylsilane and boron trifluoride etherate. This facile strategy was further used to synthesize preclamol. A highly regioselective dehydration of 3-arylpiperidin-3-ol with boron trifluoride etherate was investigated for preparing 3-aryl-1,4,5,6-tetrahydropyridine skeleton. A novel selenium dioxide mediated dihydroperoxidation of 3-aryl-1,4,5,6-tetrahydropyridine was also examined.
PHENYL SUBSTITUTED PIPERIDINE COMPOUNDS FOR USE AS PPAR ACTIVATORS
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Page 103, (2008/06/13)
PPAR alpha activators, pharmaceutical compositions containing such compounds and the use of such compounds to elevate certain plasma lipid levels, including high density lipoprotein-cholesterol and to lower certain other plasma lipid levels, such as LDL-cholesterol and triglycerides and accordingly to treat diseases which are exacerbated by low levels of HDL cholesterol and/or high levels of LDL-cholesterol and triglycerides, such as atherosclerosis and cardiovascular diseases, in mammals, including humans.
CHIRAL, POTENTIALLY IRREVERSIBLE LIGANDS FOR THE SIGMA RECEPTOR BASED ON THE STRUCTURE OF 3-(3-HYDROXYPHENYL)-N-PROPYLPIPERIDINE (3-PPP)
Grayson, Neile A.,Bowen, Wayne D.,Rice, Kenner C.
, p. 2281 - 2292 (2007/10/02)
(+)-3-PPP is an optically active, highly potent and selective ligand for sigma receptors.The resolved enantiomeric pairs of potential irreversible sigma ligands (5a,b) and (9a,b) were designed and synthesized based on the structure of 3-PPP.An improved me
PHENYL-AZACYCLOALKANES AND USE THEREOF IN TREATMENT OF CENTRAL NERVOUS SYSTEM DISORDERS
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, (2008/06/13)
Compound of the formula STR1 wherein n is 1 or 2, Y is OH, R 1 COO--, R 2 R 3 NCOO--or R 4 O whereby R 1 is an alkyl group, or a possibly substituted phenyl group, R 2 is an alkyl, phenethyl, or benzyl or phenyl group, R 3 is H or an alkyl group and R 4 i
1,3-disubstituted piperidine compounds as neuroleptic agents
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, (2008/06/13)
Certain novel 1-(substituted-alkyl)-3-(3-hydroxyphenyl)piperidine compounds, and the pharmaceutically-acceptable acid-addition salts thereof, possess pharmaceutical activity as neuroleptic agents, and they are useful for treating psychotic disorders, e.g.
3-Phenylpiperidines. Central Dopamine-Autoreceptor Stimulating Activity
Hacksell, Uli,Arvidsson, Lars-Erik,Svensson, Uno,Nilsson, J. Lars G.
, p. 1475 - 1482 (2007/10/02)
Thirty compounds related to the selective dopamine-autoreceptor agonist 3-(3-hydroxyphenyl)-N-n-propylpiperidine have been synthesized and tested for central dopamine-autoreceptor stimulating activity.The 3-(3-hydroxyphenyl)piperidine moiety seems indispensable for high potency and selectivity.Introduction of an additional hydroxyl group into the 4-position of the aromatic ring gives a compound with dopaminergic activity but lacking selectivity for autoreceptors. 3-(3-Hydroxyphenyl)-N-n-propylpyrrolidine, 3-(3-hydroxy)-N-n-propylperhydroazepine, and 3-(3-hydroxyphenyl)quinuclidine were all inactive.The most potent compounds were the N-isopropyl-, N-n-butyl-, N-n-pentyl-, and N-phenethyl-substituted 3-(3-hydroxyphenyl)piperidine derivatives.None of the compounds investigated seemed to have central noradrenaline- or serotonin-receptor stimulating activity.
