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Synthesis of 2- and 3-trifluoromethylmorpholines: useful building blocks for drug discovery

Tetrahedron , 2013, 69 (19), 3796-3804

DOI: 10.1016/j.tet.2013.03.067

Shcherbatiuk A. V.; Shyshlyk O. S.; Yarmoliuk D. V.; Shishkin O. V.; Shishkina S. V.; Starova V. S.; Zaporozhets O. A.; Zozulya S.; Moriev R.; Kravchuk O.; Manoilenko O.; Tolmachev A. A.; Mykhailiuk P. K.

2- and 3-Trifluoromethylmorpholines were prepared in racemic and optically active forms. The synthesis commenced from the commercially available 2-trifluoromethyloxirane. The elaborated procedures were scalable, and the products were obtained in multigram quantities. The obtained compounds were comprehensively characterized by crystallographic analysis, fluorescence measurements, solubility, pKa, logD parameters, and clearance rate. The potential of the synthesized amines as the building blocks for drug discovery is thus demonstrated.

Synthesis of 2- and 3-trifluoromethylmorpholines: useful building blocks for drug discovery

Shcherbatiuk A. V.; Shyshlyk O. S.; Yarmoliuk D. V.; Shishkin O. V.; Shishkina S. V.; Starova V. S.; Zaporozhets O. A.; Zozulya S.; Moriev R.; Kravchuk O.; Manoilenko O.; Tolmachev A. A.; Mykhailiuk P. K.
Tetrahedron 2013, 69 (19), 3796-3804
DOI: 10.1016/j.tet.2013.03.067

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