- Synthesis and endothelin receptor binding activity of synthetic analogues of RES-1149-2
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A direct synthesis of analogues 6 and 7 is described. The key transformations are the addition of dibromomethyl lithium to a ketone and the subsequent mild hydrolysis to a hemiacetal. (C) 2000 Elsevier Science Ltd. All rights reserved.
- Kraus, George A.,Wang, Xuemei
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p. 895 - 897
(2007/10/03)
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- Preparation, Reactivity, and Spectral Properties of 1,3-Dioxin Vinylogous Esters: Versatile β-Ketovinyl Cation Equivalents
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A full account of the preparation, reactivity, and spectral properties of three 1,3-dioxin vinylogous esters (4-6) is presented.The synthetic approach of these versatile β-ketovinyl cation equivalents involves a BF3*Et2O-promoted Prins reaction between cyclic 1,3-diketones (i.e., 1,3-cyclopentanedione, 1,3-cyclohexanedione, and 1,3-cycloheptanedione) and either formaldehyde or trioxane.The reactions explored include reductive and alkylative 1,3-ketone transpositions, affording a variety of simple β-unsubstituted and β-substituted α-hydroxymethyl α,β-enones, alkylations with carbon electrophiles, and hydroxylations with oxygen electrophiles.
- Smith, Amos B.,Dorsey, Bruce D.,Ohba, Masashi,Lupo, Andrew T.,Malamas, Michael S.
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p. 4314 - 4325
(2007/10/02)
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