Tetramethyl acetyleneurea prodn - by condensing dimethyl urea and glyoxal in presence of hydrogen chloride using water as solvent

摘要

Title cpd. (I) (i.e. 2,4,6,8-tetramethyl-2,4,6,8-tetraazabicyclo 3,3,0 octane-3,7-dione), is prepd. in better yield when the process solvent is water. Compared with use of aq. methanol solvent yields are about 87% cf. 61%; use of toxic methanol is obviated and process is suitable for large scale operation. (I) is a known neuroleptic. Specifically water is 1-5 moles per mole glyoxal.