1074-75-5Relevant articles and documents
AZETIDIN-3-YLMETHANOL DERIVATIVES AS CCR6 RECEPTOR MODULATORS
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Page/Page column 187; 190, (2021/11/06)
The present invention relates to compounds of Formula (I), their synthesis and use as CCR6 receptor modulators for the treatment or prevention of various diseases, conditions or disorders.
Palladium-catalyzed construction of poly-substituted indolizinones
Cho, Hanyang,Kim, Ikyon
experimental part, p. 5464 - 5480 (2012/09/08)
We have developed a highly efficient one-pot approach to poly-substituted indolizinones from tertiary propargylic alcohols by using a palladium-catalyzed domino reaction. This reaction is proposed to proceed via successive aminopalladation, reductive elim
An enzymatic toolbox for the kinetic resolution of 2-(Pyridin-x-yl)but-3- yn-2-ols and tertiary cyanohydrins
Nguyen, Giang-Son,Kourist, Robert,Paravidino, Monica,Hummel, Anke,Rehdorf, Jessica,Orru, Romano V. A.,Hanefeld, Ulf,Bornscheuer, Uwe T.
supporting information; experimental part, p. 2753 - 2758 (2010/07/06)
The kinetic resolution of a series of acetates of tertiary alcohols bearing a nitrogen substituent has been studied by using several recombinant carboxyl esterases and variants thereof expressed in E. coli. Most of the enzymes were active in the conversion of these tertiary alcohols and excellent enantioselectivities were achieved in the synthesis of three 2-(pyridin-x-yl)but-3-yn-2-ols with the nitrogen atom in the pyridine ring in the 2′-, 3′-, and 4′-positions. The resolution of tertiary cyanohydrins proved to be more difficult as the enantioselectivity of the enzymes was generally lower. Nevertheless, (S)-1-cyano-2,2,2-trifluoro-1- phenylethyl acetate was obtained with 99% ee. The results show that the limited substrate range of the individual enzymes in the synthesis of a series of tertiary alcohols can be efficiently overcome by using a combination of different enzymes.