7497-19-0Relevant academic research and scientific papers
Synthesis and anti-parasitic activity of C-benzylated (N-arylcarbamoyl)alkylphosphonate esters
Adeyemi, Christiana M.,Isaacs, Michelle,Mnkandhla, Dumisani,Klein, Rosalyn,Hoppe, Heinrich C.,Krause, Rui W.M.,Lobb, Kevin A.,Kaye, Perry T.
, p. 1661 - 1667 (2017/03/08)
Unexpected substituent-dependent regioselectivty challenges in the synthesis of C-benzylated (N-arylcarbamoyl)phosphonate esters have been resolved. The C-benzylated N-furfurylcarbamoyl derivative showed low micromolar PfLDH inhibition, while one of the C-benzylated N-arylcarbamoyl analogues was active against Nagana Trypanosoma brucei parasites which are responsible for African trypanosomiasis in cattle.
SUBSTITUTED PHENYLLUREAS AND PHENYLAMIDES AS VANILLOID RECEPTOR LIGANDS
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Page/Page column 116; 117, (2010/11/18)
The invention relates to substituted phenylureas and phenylamides of formula (I), to processes for the preparation thereof, to pharmaceutical compositions containing these compounds and also to the use of these compounds for preparing pharmaceutical compositions.
Vanilloid receptor ligands, pharmaceutical compositions containing them, process for making them and use thereof for treating pain and other conditions
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Page/Page column 37; 38, (2008/12/08)
Compounds corresponding to formula I: which act as vanilloid receptor ligands, pharmaceutical compositions containing such compounds, a process for the producing such compounds, and the use thereof to treat or inhibit pain and/or various other disorders or conditions.
Ligand exchange reaction of sulfoxides in organic synthesis: A novel method for generation of magnesium enolates and its application to synthesis of α-halocarboxylic acid derivatives and α-haloaldehydes
Satoh,Kitoh,Onda,Takano,Yamakawa
, p. 4957 - 4972 (2007/10/02)
A new method for synthesis of α-halo(Cl, F)carboxylic acid derivatives and α-haloaldehydes is described. α-Halo-α-sulfinyl carboxylic acid, esters, and α-halo-α-sulfinyl aldehydes were easily prepared from aryl 1-haloalkyl sulfoxides and alkyl chloroformate and ethyl formate, respectively, in good yields. α-Chloro-α-sulfinyl amides were synthesized from (p-tolylthio)acetic acid. Ligand exchange reaction of the sulfinyl group of these acids, esters, amides, and aldehydes with ethylmagnesium bromide gave the magnesium enolates, which were treated with water to give α-halocarboxylic acid derivatives and α-chloroaldehydes in good yields. The magnesium enolates derived from the α-chloro-α-sulfinyl acid derivatives were trapped with carbonyl compounds to afford the adducts, which were transformed to α,β-epoxy carboxylic acid derivatives. Thermal elimination of the sulfinyl group in the α-halo-α-sulfinyl acid derivatives and the α-halo-sulfinyl aldehydes gave α-halo-α,β-unsaturated carboxylic acid derivatives and α-halo-α,β-unsaturated aldehydes in high yields.
A ONE-POT PREPARATION OF α-HALO-CARBONYL AND α-HALO-SULFONYL COMPOUNDS BY HALO-DEACYLATION
Mignani, G.,Morel, D.,Grass, F.
, p. 5505 - 5508 (2007/10/02)
The reaction of β-ketoesters, β-diketones and β-sulfonylketones with N-halosuccinimides in the presence of a base gives α-halo-carbonyl and α-halo-sulfonyl derivatives by a one-pot halo-deacylation reaction.A facile synthesis of pseudo-ionone is described.
Direct Conversion of Arylamines to the Halides by Deamination with Thionitrite or Related Compounds and Anhydrous Copper(II) Halides
Oae, Shigeru,Shinhama, Koichi,Kim, Yong Hae
, p. 1065 - 1069 (2007/10/02)
Reactions of various arylamines with either t-butyl thionitrite, t-butyl thionitrate, or p-toluenesulfonyl nitrite in the presence of anhydrous copper(II) halides under mild conditions gave corresponding aryl halides in good yields.This reaction in the presence of such olefins as acrylonitrile, styrene, and acrylic acid gave the corresponding 2-aryl-1-haloethanes as the main products. t-Butyl thionitrite, t-butyl thionitrate, and p-toluenesulfonyl nitrite were found to be better deaminative reagents than alkyl nitrites or alkyl nitrates due to their weak sulfur-nitrogen bonds.
