Bacteriostats. VII. Substituted Benzylphenols¹

Computationally-Guided Optimization of a Docking Hit to Yield Catechol Diethers as Potent Anti-HIV Agents

“…Ultimately, the synthetic efforts focused on the preparation of diphenylmethanes (Scheme ) and catechol diethers (Schemes –). The o -benzylphenols in Scheme arose from Friedel–Crafts reactions of arylmethyl halides or alcohols with phenols. , The catechol ether intermediates were prepared from substituted phenols and the aryl fluorides using S N Ar reactions followed by treatment with boron tribromide or lithium chloride (Schemes and ). The final compounds were prepared in a two-step sequence via the Mitsunobu reaction to install the bromoethoxy linker, followed by 2,4-bis­(trimethylsiloxy)­pyrimidine alkylation ( 5 – 15 and 20 – 32 ) …”

Syntheses ofN‐[3‐(1‐methyl‐1H‐2‐imidazolyl)propyl]benzamides andN‐[3‐(1‐methyl‐1H‐2‐imidazolyl)propyl]benzenesulfonamides

“…Reaction of potassium phthalimide (1) with 4-bromobutyronitrile in dimethyl formamide gave 4-(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)butyronitrile (3) in 78% yield [19]. Compound 3 was converted to [3-(1H-imidazol-2-yl)propyl]-1H-isoindole-1,3(2H)-dione (5) by a known procedure [20].…”

Syntheses and Antimicrobial Properties of Isothiocyanate Derivatives

“…Earlier in vitro studies with an everted gut preparation indicated that the transport of phenoxymethyl penicillin and phenoxybenzyl penicillin (phenbenicillin) is a saturable process (5, 6), although additional studies did not produce evidence of active transport (6).…”