摘要 |
<p>Sulphonyl-amidines of formula (I), in which A is a 5-6 member heterocycle e.g. pyridyl or furonyl, opt. substd. by lower alkyl, R1 is opt. substd. sulphonyl and R2 is H or lower alkyl, are made by (a) reacting an alkyl-imidate (II) in which R3 and R4 are alkyl, aryl or aralkyl, with a sulphamide to obtain a sulphite (III); (b) per-acid oxidn. to a sulphoxide; (c) reacting with an amine base to give a N-sulphonyl acrylamidine; and (d) reacting with a heterocyclic thiol A-(CH2)m-SH.</p> |