Sequential acetic acid-sodium chloride treatment to control salt stoichiometry of a hydrochloride salt
The sequential treatment of an intermediate in the synthesis of GSK159797 with a protic acid and sodium chloride was developed to control the stoichiometry of the hydrochloric acid salt of the API. This offered significant advantages over addition of hydrochloric acid, thus avoiding decomposition of an acid-sensitive formamide group. A range of acids were investigated to determine the optimum pKa range in which to use the acid. The optimum process, using acetic acid, was performed on >100 kg input scale.
Caine, Darren M.,Paternoster, Ian L.,Sedehizadeh, Simon,Shapland, Peter D. P.
experimental part
p. 518 - 523
(2012/08/13)
CHEMICAL PROCESS AND NEW CRYSTALLINE FORM
The present invention relates to the preparation of a ?2 adrenergic agonist in crystalline salt form. In particular the invention relates to preparation of a crystalline salt of compound (I): in particular a crystalline monohydrochloride salt. The inventi
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Page/Page column 28-29
(2010/02/14)
Crystalline form of beta2 adrenergic receptor agonist
The invention provides a novel β2 adrenergic receptor agonist in crystalline salt form. The invention also provides pharmaceutical compositions comprising the novel β2 adrenergic receptor agonist in crystalline salt form, formulation
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Page 13
(2008/06/13)
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