1124174-16-8Relevant articles and documents
A biocatalytic/reductive etherification approach to substituted piperidinyl ethers
Kuethe, Jeffrey T.,Janey, Jacob M.,Truppo, Matthew,Arredondo, Juan,Li, Tao,Yong, Kelvin,He, Shuwen
, p. 4563 - 4570 (2014/06/10)
A synthetically useful protocol has been developed for the preparation of highly functionalized piperidinyl ethers. Biocatalytic reduction of cyclhexanones 7, 10, and 14 allows for the preparation of both cis- and trans diastereomers with an extremely high degree of stereochemical control. Reductive etherification of the corresponding trimethylsilylethers with 1-(benzyloxycarbonyl)-4-piperidinone 17 in the presence of triethylsilane and catalytic TMSO-Tf provides the desired piperidinyl ethers in good to excellent yields. Finally hygrogenolysis of the nitrogen protecting group leads to piperidinyl ethers in near quantitative yields. Application of the methodology to a range of piperidinyl ethers, including the core scaffolds of diphenylpyraline and ebastine, is also described.
NOVEL TETRAHYDROISOQUINOLINE COMPOUNDS
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, (2012/07/14)
The present invention relates to a compound or a pharmacologically acceptable salt thereof having an excellent DGAT inhibitory effect and feeding suppressant effect. The present invention provides trans-6-[3-(2,4-difluoro-phenyl)-ureido]-3,4-dihydro-1H-is