ChemInform Abstract: An Improved Synthesis of Enantiomerically Pure RWJ 69442, a Development Candidate for the Treatment of Benign Prostatic Hyperplasia

Autor: Gee-Hong Kuo, Prouty Catherine P, William V. Murray, Rekha D. Shah
Rok vydání: 2010
Předmět:
Zdroj: ChemInform. 32
ISSN: 1522-2667
0931-7597
Popis: This report describes an improved synthesis of enantiomerically pure (S)-2-[4-(Dimethylamino)phenyl]-2,3-dihydro-N-[2-hydroxy-3-[4-[2-(1-methylethoxy)-phenyl]-1-piperazinyl]propyl]-1,3-dioxo-1H-isoindole-5-carboxamide (RWJ 69442), a potent and selective αla-adrenergic receptor antagonist for the treatment of benign prostatic hyperplasia. The synthesis highlights less hazardous reagents, easier purification and higher enantiomeric purity. The N-benzyl-N—t-butoxycarbonyl amine 6 could serve as an enantiomerically pure chiral building block for asymmetric synthesis.
Databáze: OpenAIRE