181115-01-5Relevant academic research and scientific papers
Highly Chemoselective gem-Difluoropropargylation of Aliphatic Alcohols
Okamura, Toshitaka,Egoshi, Syusuke,Dodo, Kosuke,Sodeoka, Mikiko,Iwabuchi, Yoshiharu,Kanoh, Naoki
supporting information, p. 16002 - 16006 (2019/11/19)
Despite the potential of α-fluoroethers in medicinal chemistry, their synthetic methods, especially etherification of aliphatic alcohols, have been limited. Herein, we developed two- and three-step gem-difluoropropargylation of aliphatic alcohols includin
PHENYL-ALKYL PIPERAZINES HAVING TNF-MODULATING ACTIVITY, PREPARATION METHOD, AND THERAPEUTIC USE THEREOF
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Page/Page column 5, (2011/06/26)
The present invention relates to phenyl-alkyl piperazines of formula (I): in which A, R1, R2 and R3 are as defined herein, having TNF-modulating activity. The invention also relates to the preparation thereof, pharmaceutical compositions thereof, and to t
INHIBITORS OF THE RENAL OUTER MEDULLARY POTASSIUM CHANNEL
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Page/Page column 76, (2010/11/18)
This invention relates to compounds having structural Formula I: and pharmaceutically acceptable salts thereof which are inhibitors of the Renal Outer Medullary Potassium (ROMK) channel (Kir1.1). The compounds of Formula I are useful as diuretics and natriuretics and therefore are useful for the therapy and prophylaxis of disorders resulting from excessive salt and water retention, including cardiovascular diseases such as hypertension and chronic and acute heart failure
Azidosubstituted arylboronic acids: Synthesis and Suzuki-Miyaura cross-coupling reactions
Sviridov, Sergey I.,Vasil'ev, Andrei A.,Sergovskaya, Natalia L.,Chirskaya, Marina V.,Shorshnev, Sergey V.
, p. 2639 - 2647 (2007/10/03)
Arylboronic acids having a remote azido group were prepared from the corresponding azidosubstituted aryl bromides via lithiation and treatment with trialkyl borates. Preparative yields were achieved when the starting aryl bromides possessed ortho-alkoxy groups, which would stabilize the intermediate aryllithium species. Conventional Suzuki cross-coupling of the arylboronic acids proceeded generally well with retention of azido group; however, sometimes azidomethyl fragment underwent oxidative transformation into a nitrile.
Catalyst ligands, catalytic metal complexes and processes using same
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, (2008/06/13)
New ligands having a backbone comprised of NCCX can be combined with a metal or metal precursor compound or formed into a metal-ligand complex to catalyze a number of different chemical transformations, including polymerization.
2,3-benzodiazepine derivatives and their use as AMPA-receptor inhibitors
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, (2008/06/13)
A compound of formula I in which X means hydrogen or halogen, Y means —NR3— or —N═, R1and R2are the same or different and mean hydrogen, C1-C6alkyl, nitro, halogen, the group —NR8R9/s
Substituent Effects. XVI. Acetolysis of 2-Phenylethyl Tosylates
Fujio, Mizue,Funatsu, Kimito,Goto, Mutsuo,Seki, Yoji,Mishima, Masaaki,Tsuno, Yuho
, p. 1091 - 1096 (2007/10/02)
The acetolysis rates of 2-arylethyl tosylates were determined for a series of aryl substituents.The non-linear substituent effect was reasonably accounted for on the basis of two linear LArSR relationships; one for the aryl-assisted (FkΔ) and one for the unassisted (Ks) process, respectively.A precise dissection of the apparent substituent effect into individual effects for both processes was achieved in this manner.The substituent effect on the ks process can be described as a linear function of ?0 with a small ρs of -0.19, and that on the FkΔ process in terms of the LArSR Eq., with a ρΔ=-3.87 and an rΔ=0.631.The use of ?+ for the FkΔ process failed to give any reasonable dissection.The r value for this FkΔ process is essentially identical to that for the neophyl solvolysis.The unique r value oh 0.6 is concluded to be characteristic of β-aryl-assisted ionization processes in general.
