Search results for "Thiazepine"
showing 2 items of 12 documents
Preparation and Structures of Isoindolone- or Pyrimidone-Condensed Heterocycles Containing a Hydroxy Group on a Cyclohexane or Norbornane Moiety
2009
With DL-valinol, 3-amino-1-propanol and o-aminothiophenol, aroyl(bi/tri)cyclic lactones 1 and 2 were cy- clized to isoindole- 4-6, 8, 9, pyrimidinone- 10 or thiazepine- 7 condensed heterocycles. The ketal lactone 3 furnished the benzthiazoloisoindole 9 and mixtures of epimeric hydroxyphthalazinoquinazolinones 11 and 12. The structures were es- tablished by means of 1 H and 13 C NMR spectroscopy and in some cases by X-ray crystallography.
The effect of pH on polymorph formation of the pharmaceutically active compound tianeptine.
2012
The anti-depressant pharmaceutical tianeptine has been investigated to determine the dynamics of polymorph formation under various pH conditions. By varying the pH two crystalline polymorphs were isolated. The molecular and crystal structures have been determined to identify the two polymorphs. One polymorph is an amino carboxylic acid and the other polymorph is a zwitterion. In the solid state the tianeptine moieties are bonded through hydrogen bonds. The zwitterion was found to be less stable and transformed to the acid form. During this investigation an amorphous form was identified.