The worldwide threat from tuberculosis (TB) has resulted in great demand for new drugs, particularly those that can treat multidrug-resistant TB. We synthesized novel pleuromutilin derivatives with N-benzylamine side chain substituted at the C14 position and evaluated their activity in vitro against a virulent strain of Mycobacterium tuberculosis (H37Rv). The primary assay results showed that five compounds inhibited the H37Rv at 20 μM, with a MIC of one of the analogues as low as 7.2 μM.

The solubility of racemic potassium 2-(1-hydroxypentyl)-benzoate (dl-PHPB) in methanol, ethanol, n-propanol, isopropyl alcohol, ethyl acetate, and acetone from 298.15 to 333.15 K was measured by an equilibrium method. The solubility data of dl-PHPB in six different solvents was correlated by the modified Apelblat equation. The correlation coefficients were observed in the range of 0.993 to 0.998, indicating a good fit. The results showed that the mole fraction solubility of dl-PHPB in methanol (6.22 × 10–2), ethanol (2.58 × 10–2), n-propanol (2.39 × 10–2), and isopropyl alcohol (6.72 × 10–3) was significantly higher than in acetone (2.58 × 10–4) and ethyl acetate (8.02 × 10–5) at 298.15 K. The experiment data would be useful for optimizing purification and recrystallization processes of dl-PHPB in industry.

Tetranitrodimerglycoluril (TNDGU) is a newly developed insensitive energetic material. Its solubility in methanol, propanone, ethyl ethanoate, and ethanenitrile between 293.15 K and 313.15 K at atmospheric pressure was investigated by the gravimetric method. The order of the solubility of TNDGU is ethanenitrile > ethyl ethanoate ≈ propanone > methanol. The solubility of TNDGU increased with an increase of temperature. The enthalpy of dissolution in each solvent was also calculated according to a modified van’t Hoff equation; the values are 25.18 kJ·mol–1 for methanol, 41.26 kJ·mol–1 for propanone, 34.70 kJ·mol–1 for ethyl ethanoate, and 36.33 kJ·mol–1 for ethanenitrile, respectively.

This paper presents the amination reactions of electron deficient aryl chlorides promoted by Mg(OH)2 without transition metals. Only using stoichiometric amount of nano sized Mg(OH)2, good to moderate isolated yields could be achieved in N-methylpyrrolidone (NMP) after 24 h at 150 °C.