| 摘要 |
<p>Cpd. of formula (I) is made by (a) reacting 3-methylthio propionitrile with methanol and gaseous HCl to obtain methyl 3-methylthio propionimidate; (b) reacting this with sulphamide in ethanol under reflux for 20-40 hours to obtain the sulphide; (c) oxidn. with a per acid, e.g. m-chloro perbenzoic or peracetic acid in a methanol/chloroform mixt. at 0-50 deg.C for 0.5-5 hrs., to give the sulphoxide; (d) reacting with a small excess of tert. amine, e.g. triethylamine, in ethanol under reflux for 0.5-3 days to obtain the N-sulphamyl acrylamidine; and (e) reacting with a heterocyclic cpd. in a solvent e.g. methanol at 0 deg.C to ambient temp. for 1 min. to 4 hours, to give (I).</p> |
