A redetermination of the crystal structure of minodronic acid monohydrate was carried out in order to provide accurate atomic coordinates and geometry information, whose knowledge is fundamental to elucidate the presumed polymorphism of the compound at room temperature.
A very efficient, cost-effective,
and easily scalable process for
the synthesis of lofexidine hydrochloride (1), an alpha
2-adrenergic receptor agonist used for treating opioid withdrawal
is presented. Process development allows the preparation of lofexidine
hydrochloride (1) through a one-pot amidation/imidazoline
ring formation reaction, starting from ethyl 2-(2,6-dichlorophenoxy)propionate
(13) and ethylenediamine (5) by the action
of titanium isopropoxide. The required intermediate ethyl 2-(2,6-dichlorophenoxy)propionate
(13) can efficiently be obtained through O-alkylation of 2,6-dichlorophenol (2) with ethyl 2-chloropropionate
(12) using potassium carbonate as an acid-scavenger agent.
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