Synthesis and endothelin receptor binding activity of synthetic analogues of RES-1149-2.
A direct synthesis of analogues 6 and 7 is described. The key transformations are the addition of dibromomethyl lithium to a ketone and the subsequent mild hydrolysis to a hemiacetal.
Kraus
G A
GA
Department of Chemistry, Iowa State University, Ames 50011, USA. gakraus@iastate.edu
Wang
X
X
D000097:Acetonitriles; D000215:Acylation; D000818:Animals; D065128:Endothelin Receptor Antagonists; D006801:Humans; D066298:In Vitro Techniques; D011817:Rabbits; D044022:Receptor, Endothelin A; D044023:Receptor, Endothelin B; D013764:Tetrahydronaphthalenes / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*
D000097:Acetonitriles; D065128:Endothelin Receptor Antagonists; C098352:RES 1149-2; D044022:Receptor, Endothelin A; D044023:Receptor, Endothelin B; D013764:Tetrahydronaphthalenes