An easy and high-yield route for the preparation of functional and chi
ral hexahydropyrimido[1,2-a]pyrimidines 3 is described. Starting from
known methioninol and 2-methylmercaptotetrahydropyrimidine 5, the targ
et compounds, which may be useful as building blocks in the synthesis
of polymodular molecular hosts, were obtained in over 50 % total yield
. As an example the iodo compound 20 was converted into the homoargini
ne analog 22 in 70 % yield.