76481-34-0Relevant academic research and scientific papers
Triphosgene and DMAP as Mild Reagents for Chemoselective Dehydration of Tertiary Alcohols
Ganiu, Moshood O.,Cleveland, Alexander H.,Paul, Jarrod L.,Kartika, Rendy
supporting information, p. 5611 - 5615 (2019/08/01)
The utility of triphosgene and DMAP as mild reagents for chemoselective dehydration of tertiary alcohols is reported. Performed in dichloromethane at room temperature, this reaction is readily tolerated by a broad scope of substrates, yielding alkenes preferentially with the (E)-geometry. While formation of the Hofmann products is generally favored, a dramatic change in alkene selectivity toward the Zaitzev products is observed when the reaction is carried out in dichloroethane at reflux.
Synthesis and pharmacological evaluation of 1-Alkyl-N-[(1R)-1-(4- fluorophenyl)-2-methylpropyl]piperidine-4-carboxamide derivatives as novel antihypertensive agents
Watanuki, Susumu,Matsuura, Keisuke,Tomura, Yuichi,Okada, Minoru,Okazaki, Toshio,Ohta, Mitsuaki,Tsukamoto, Shin-Ichi
experimental part, p. 1376 - 1385 (2012/01/05)
We synthesized and evaluated inhibitory activity against T-type Ca 2+ channels for a series of 1-alkyl-N- [(1R)-1-(4-fluorophenyl)-2- methylpropyl]piperidine-4-carboxamide derivatives. Structure-activity relationship studies have revealed that the isopropyl substituent at the benzylic position plays an important role in exerting potent inhibitory activity, and the absolute configuration of the benzylic position was found to be opposite that of mibefradil, which was first launched as a new class of T-type Ca2+ channel blocker. Oral administration of N- [(1R)-1-(4-fluorophenyl)-2-methylpropyl]-1-[2-(3-methoxyphenyl)ethyl] piperidine-4-carboxamide (17f) lowered blood pressure in spontaneously hypertensive rats without inducing reflex tachycardia, an adverse effect often caused by traditional L-type Ca2+ channel blockers.
Application of a 3,3-diphenylpentane skeleton as a multi-template for creation of HMG-CoA reductase inhibitors
Hosoda, Shinnosuke,Matsuda, Daisuke,Tomoda, Hiroshi,Hashimoto, Mariko,Aoyama, Hiroshi,Hashimoto, Yuichi
scheme or table, p. 4228 - 4231 (2010/05/02)
Based on our hypothesis that the 3,3-diphenylpentane (DPP) skeleton is useful as a multi-template for creation of various biologically active compounds and acts as a steroid skeleton substitute, we designed and synthesized novel HMG-CoA reductase inhibitors with a DPP skeleton. Among them, sodium (E,3R,5S)-7-(2-(4-fluorophenyl)-4-(3-phenylpentan-3-yl)phenyl)-3,5-dihydroxy-hept-6-enoate showed potent HMG-CoA reductase-inhibitory activity comparable with that of clinically useful mevastatin.
VITAMIN D RECEPTOR MODULATORS
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Page/Page column 128-129, (2008/06/13)
The present invention relates to novel, non-secosteroidal, phenyl-benzothiophene compounds with vitamin D receptor (VDR) modulating activity that are less hypercalcemic than 1α,25 dihydroxy vitamin D3. These compounds are useful for treating bone disease
INDOLE-DERIVATIVE MODULATORS OF STEROID HORMONE NUCLEAR RECEPTORS
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Page 72, (2010/02/07)
The present invention provides a compound of formula I or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising an effective amount of a compound of Formula I in combination with a suitable carrier, diluent, or excipient, and methods for treating physiological disorders, particularly congestive heart disease, comprising administering to a patient in thereof an effective amount of a compound of Formula I.
Arene-catalysed lithiation of fluoroarenes
Guijarro, David,Yus, Miguel
, p. 1135 - 1138 (2007/10/03)
The reaction of different fluoroarenes 1 with lithium and a catalytic amount (7%) of naphthalene in THF at -30°C affords the corresponding aryllithium intermediates which, by reaction with several electrophiles at temperatures ranging between -30 and 0°C, lead to the expected products 2, after hydrolysis. (C) 2000 Elsevier Science Ltd.
Transition-State Polarization in Cleavage of C-C Bonds in Radical Anions
Maslak, Przemyslaw,Narvaez, Javier N.,Kula, Jozef,Malinski, David S.
, p. 4550 - 4559 (2007/10/02)
The substituent effect on the rate of C-C bond cleavage in radical anions of 1-(4-nitrophenyl)-2-(substituted-phenyl)-1,1,2,2-tetraethylethanes has been explored.The data provide evidence for two distinctive modes of bond scission.One mode is characterized by a significant negative charge transfer across the scissile bond in the transition state.Such polarization of the transition state is in contradiction to the prediction based on the fragments' stability.The second mode, dominant in cases where the charge shift leads to negative charge accumulation on an already electron-rich fragment, involves a ?* radical anion.Both modes point to a general kinetic preference for a cleavage of radical anions that allows for charge delocalization across the scissile bond.
