A facile two-step method for the construction of fused pyrrole ring leading to 5-substituted 2,3-dihydro-1H-pyrrolo[3,2,1-ij]quinolin-1-ones via C-C followed by intramolecular C-N bond forming reaction is described. In vitro pharmacological evaluation and molecular modelling studies of some of the compounds synthesized are presented.
SummaryA two step synthesis of 2-alkynyl-4-arylquinolines has been accomplished via Pd/C-mediated regioselective C-2 alkynylation of 2,4-dichloroquinoline in water followed by Suzuki coupling at C-4 of the resulting 4-chloro derivative.
An efficient, commercially viable and safe process for
the preparation of losartan potassium, an antihypertensive drug substance,
with an overall yield of 55.5% and ∼99.9% purity (including
five chemical reactions and two recrystallizations) and meeting all
other regulatory requirements is described. Formation and control
of all the possible impurities are also described.
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