827605-45-8Relevant articles and documents
Concise synthesis of a selective α1-adrenoceptor antagonist
Connolly, Terrence J.,Matchett, Michael,McGarry, Patrick,Sukhtankar, Sunil,Zhu, Jiang
, p. 391 - 397 (2006)
An efficient synthesis of an adrenoceptor antagonist has been developed and demonstrated in a pilot plant. A linear synthesis that relied on a catalytic reduction of a rather insoluble nitroaromatic proved to be a viable route. The active pharmaceutical ingredient (API) that contained an amidine functional group was generated from the amino-containing precursor by activation of dimethylacetamide (DMA) with phosphorus oxychloride (POCl3). The reaction between DMA and POCl3 was studied using ReactIR and was found to be a fast but not instantaneous reaction. The iminium salt generated from DMA and POCl3 had acceptable stability to allow for its use on a pilot-plant scale; however, a trend towards decomposition was revealed on the basis of in situ FTIR data. Formation of the complex was evaluated in a reaction calorimeter (RC-1), and the stability of the complex was probed with an Advanced Reactive System Screening Tool (ARSST).
ARYLAMINE-SUBSTITUTED QUINAZOLINONE COMPOUNDS
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Page 63, (2010/02/10)
Compounds represented by Formula (I) which are useful as are alpha-1A/B adrenoceptor antagonists, to methods of treating conditions associated with the activity of alpha-1A/B adrenoceptors, and to methods of making said compounds, wherein Ar, Z, R, R', R