Galderma RandD les Templiers

Sophia, France

Galderma RandD les Templiers

Sophia, France

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Tabet S.,Galderma RandD les Templiers | Rodeville N.,Galderma RandD les Templiers | Boiteau J.-G.,Galderma RandD les Templiers | Cardinaud I.,Galderma RandD les Templiers
Organic Process Research and Development | Year: 2016

An improved process for tert-butanesulfinyl ketimines formation using titanium(IV) alkoxides is described. This new protocol gives better results especially for sterically hindered ketones compared to classical conditions where titanium(IV) isopropoxide is found to be only moderately effective. We found that removal of isopropanol or ethanol from the reaction mixture either under a nitrogen flow or under vacuum dramatically increased reaction rate, extent of conversion, and yield of the reaction. This methodology has been exemplified on several substrates reported in the literature to be difficult. © 2016 American Chemical Society.


Boiteau J.-G.,Galderma RandD les Templiers | Rodeville N.,Galderma RandD les Templiers | Martin C.,Galderma RandD les Templiers | Tabet S.,Galderma RandD les Templiers | And 4 more authors.
Organic Process Research and Development | Year: 2015

Herein, we report the kilogram-scale synthesis of CD08108, a novel MC1R agonist. This synthesis has been developed to produce the first batches of this compound for preclinical and clinical studies. Two amido couplings were used to synthesize the backbone of the API. Improvements have been made to isolate crystalline intermediates and to remove all column chromatographic steps. Crystallization of the final API was monitored by DSC in-process control during slurry ripening of the amorphous suspension of the hydrochloride salt. © 2015 American Chemical Society.

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