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Synthesis of 14C-labelled CGS 16949A (Fadrozole HCl), a potent aromatase inhibitor

โœ Scribed by Bohdan Markus; Alban J. Allentoff; Mahesh Desai; Naba K. Chaudhuri; Timothy Duelfer


Publisher
John Wiley and Sons
Year
1997
Tongue
French
Weight
318 KB
Volume
39
Category
Article
ISSN
0022-2135

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## Background: Fadrozole hydrochloride (cgs 16949a) is a highly potent, nonsteroidal aromatase inhibitor that significantly lowers estrogen levels in postmenopausal women and can be effective therapy for patients with advanced hormone-dependent breast carcinoma. circulating estradiol, estrone, and

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CGS 19755 is a selective NMDA (N-methyl-D-aspartate) antagonist presently under development as a neuronal protecting agent after stroke and head trauma. It was synthesized with 1%-labelling in the carboxylic acid side chain via the synthetic route displayed in Scheme 1. Key steps in the synthesis in