| 摘要 |
<p>1-(1-(4-Diphenylmethyl piperazinyl)) 3-(1-(1,3-dihydrobenzo 1,3-diazolyl-2-one))propane is made by (a) reacting a cpd. of formula (I) with a lower alkyl chloroformate in a high-boiling inert solvent at over 120 deg.C for 12-72 hrs. to obtain (II); (b) reacting this with 4-diphenylmethyl piperazine to obtain a o-nitro aniline (III); (c) reducing this with boron hydride, aluminium hydride or a transition metal in presence of a proton donor and a Pd/C catalyst to give (IV); and (d) cyclising to obtain the required prod. by heating under low vacuum to atmos. pressure with a drying agent at 160-180 deg.C. X is halogen and R is methyl or ethyl.</p> |
