Conglomerate formative precursor of chiral drug timolol: 3-(4-Morpholino-1,2,5-thiadiazol-3-yloxy)-propane-1,2-diol

摘要: Abstract Solid state properties of 3-(4-N-morpholino-1,2,5-thiadiazol-3-yloxy)-propane-1,2-diol 3 , the synthetic precursor popular drug timolol, have been investigated. The original solubility test, data X-ray diffraction and DSC methods indicate that compound is prone to spontaneous resolution. Diol crystallizing from both enantiopure or racemic feed material forms “guaifenesin-like” crystal packing in which classic H-bonded bilayers, framed sides by hydrophobic molecular fragments, act as basic supramolecular motif. main chain conformation molecules crystals diol differs guaifenesin crystals, this fact changes absolute configuration spiral columns formed intermolecular hydrogen bonds compared with crystals.