Efficient and scalable synthesis of thiazole fused benzazepine as a D2 partial agonist

…, W Blackwell, G Steelman, J Hulsizer, RA Urbanek

Index: Xiong, Hui; Wu, Ye; Lehr, Scott G.; Blackwell, William; Steelman, Gary; Hulsizer, Jim; Urbanek, Rebecca A. Tetrahedron Letters, 2012 ,  vol. 53,  # 44  p. 5833 - 5836,4

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Citation Number: 4

Abstract

The development of an efficient and scalable synthetic route to prepare the selective D2 partial agonist (1) is described here. Regioselective nitration of tetrahydrobenzazepine 2, followed by reductive amination, hydrogenation, and oxidative cyclization afforded 1 in good yield, without the need of column chromatography.