ON THE REGIOCHEMISTRY OF THE ALKYLATION OF TERT-BUTYL -BUTYL-1,2-DIHYDRO-2-OXO-3-PYRIDYLMETHYL]CARBAMATE - PRECURSOR OF A SERIES OF POTENT ANGIOTENSIN-II RECEPTOR ANTAGONISTS
T. Koppe et al., ON THE REGIOCHEMISTRY OF THE ALKYLATION OF TERT-BUTYL -BUTYL-1,2-DIHYDRO-2-OXO-3-PYRIDYLMETHYL]CARBAMATE - PRECURSOR OF A SERIES OF POTENT ANGIOTENSIN-II RECEPTOR ANTAGONISTS, Tetrahedron letters, 36(3), 1995, pp. 377-380
The key intermediate 5 of a large number of potent AT(1) selective ang
iotensin II antagonists e.g. the potent cyclopropylmethyl derivative 1
(EMD 69943) was synthesized by regioselective alkylation of carbamate
3 with the well-known 4'-(bromomethyl)biphenyl-2-carbonitrile (4) and
n-butyllithium as the preferred base.