Patent ID: 6258976
Filing Date: 2001-07-10
Classification: C07C,Y02P

Abstract:
A process for producing a compound of formula (II)H.sub.2 N--(CH.sub.2).sub.n --NH--C(.dbd.NR.sup.1)--NH--(CH.sub.2).sub.m --NH.sub.2 (II),wherein n and m are each independently an integer from 2 to 8; and R.sup.1 is a protecting group having a carbonyl group, the process comprising:(a) reacting a compound of formula (V)NC--(CH.sub.2).sub.n-1 --N.dbd.C.dbd.S (V),wherein n is as described above, with ammonia;(b) protecting the compound of formula (V) with a protecting group having a carbonyl group, to produce a compound of formula (VI)NC--(CH.sub.2).sub.n-1 --NHC(.dbd.S)NH--Prot (VI),wherein n is as described above and Prot is the protecting group;(c) coupling the compound of formula (VI) with a compound of formula (VII)H.sub.2 N--(CH.sub.2).sub.m --NHC--Bas (VII),wherein m is as described above and Bas is a basic labile group;(d) hydrolyzing the basic labile group, to produce a compound of formula (VIII)NC--(CH.sub.2).sub.n-1 --NH--C(.dbd.N--Prot)--NH--(CH.sub.2).sub.m --NH.sub.2 (VIII),wherein n, m and Prot are as described above; and(e) reducing the nitrile group in the compound of formula (VIII), to produce a compound of formula (II).