177036-78-1Relevant articles and documents
PROCESS FOR THE PREPARATION OF AN ENDOTHELIN RECEPTOR ANTAGONIST
-
Page/Page column 25, (2013/05/09)
The present invention relates to a novel process for the preparation of a compound of formula (I) wherein R is a methyl or methoxy group; to certain novel intermediates prepared in such a process and their use.
Kinetic resolution of racemic α-tert-alkyl-α-hydroxy esters by enantiomer-selective carbamoylation
Kurono, Nobuhito,Ohtsuga, Kentaro,Wakabayashi, Masanori,Kondo, Tadahiro,Ooka, Hirohito,Ohkuma, Takeshi
experimental part, p. 10312 - 10318 (2012/01/30)
Kinetic resolution of sterically hindered racemic α-tert-alkyl- α-hydroxy esters is performed by enantiomer-selective carbamoylation with the t-Bu-Box-Cu(II) catalyst (Box = bis-(oxazoline)). The reaction with 0.5 equiv of n-C3H7NCO is carried out with a substrate-to-catalyst molar ratio of 500-5000 at -20 to 25 °C. The high enantiomer-discrimination ability of the catalyst achieves an excellent stereoselectivity factor (s = kfast/kslow) of 261 in the best case. A catalytic cycle for this reaction is proposed (Figure presented).
Azinyloxy, and phenoxy-diaryl-carboxylic acid derivatives, their preparation and use as mixed ETA/ETB endothelin receptor antagonists
-
Page column 16, (2010/02/05)
The invention relates to carboxylic acid derivatives of the formula I where the radicals have the meanings stated in the description, and to their use as drugs.