348579-13-5Relevant academic research and scientific papers
GONADOTROPIN-RELEASING HORMONE RECEPTOR ANTAGONISTS AND METHODS RELATING THERETO
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Page/Page column 86, (2008/12/04)
GnRH receptor antagonists are disclosed which have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure, wherein R1a, R1b, R1c, R1d, R2, R2a, and A are as defined herein, including stereoisomers, esters, solvates and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.
The synthesis of N-arylcyclopropylamines via palladium-catalyzed C-N bond formation
Cui, Wenge,Loeppky, Richard N
, p. 2953 - 2956 (2007/10/03)
A variety of N-arylcyclopropylamines has been prepared in one step, by the Pd2(dba)3/BINAP/NaOtBu-catalyzed amination of an aryl bromide with cyclopropylamine. Compounds bearing the N-aryl substitutent (phenyl, 4-methylphenyl, 2-methoxyphenyl, 3-methoxyphenyl, 4-chlorophenyl, 1-napthyl, 9-anthryl, 9-phenanthryl, and 3-pyridyl) were prepared in isolated yields ranging from 43 to 99%. Overall, this chemistry represents a vast improvement over the previous multi-step procedures for the synthesis of compounds of this type.
