A general approach to homochiral alpha-amino substituted bromo-heteroaromatics suitable for two-dimensional rapid analogue synthesis

作者：Schultz Fademrecht Carsten; Kinzel Olaf^*; Marko Isvan E; Pospisil Tomas; Pesci Silvia; Rowley Michael; Jones Philip

来源：Tetrahedron, 2009, 65(45): 9487-9493.

DOI：10.1016/j.tet.2009.08.013

An efficient and general synthesis of homochiral alpha-amino substituted bromo-heteroaromatics B using a diastereoselective 1,2-addition has been developed. The obtained heteroaromatic intermediates allow for a rapid two-dimensional exploration of a new series of histone deacetylase inhibitors, through Suzuki-Miyaura cross-coupling reactions for the introduction of a second aromatic element, followed by global deprotection and derivatization of the amino group.

• 出版日期2009-11-7