K. Srinivasulu, M. A. Kumar, C. N. Raju
Aug 13, 2007
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0
Influential Citations
7
Citations
Journal
Arkivoc
Abstract
Novel 2-substituted-3,4-dihydro-1-(9H-carbazol-4-yloxy)methyl-3-(2-(2-methoxyphenoxy) ethyl)-1,3,2λ 5 -oxazaphosphole 2-oxides (3a-e) were synthesized by condensation of 1-(9H- carbazol-4-yloxy)-3-(2-(2-methoxy phenoxy)ethylamino)propan-2-ol (1) (carvedilol) with dichlorides of aryl phosphorodichloridates / N,N-bis(2-chloroethyl)phosphoramidic dichloride (2a-e) in the presence of triethylamine at 40 to 45 °C. The other title compounds (6a-c, and 6d-f) were prepared in two steps. In the first step, dichlorophenylphosphine/ethyl phosphorodichloridite was reacted with 1 in the presence of Et3N to give the corresponding P(III) intermediates (5a,b) in N2 atmosphere. In the second step, 5a,b were treated with H2O2, S or Se to convert them to the corresponding P(V) state (6a-c, 6d-f). Compounds 3a-e, 6a-f were screened for antifungal and antibacterial activity. Most of these compounds exhibited moderate activity.