- IMIDAZOPYRIDINE MACROCYCLES AS INHIBITORS OF HUMAN IMMUNODEFICIENCY VIRUS REPLICATION
-
Disclosed are compounds of Formula (I), including pharmaceutically acceptable salts, pharmaceutical compositions comprising the compounds, methods for making the compounds and their use in inhibiting HIV integrase and treating those infected with HIV or AIDS.
- -
-
Page/Page column 38; 39
(2017/03/08)
-
- PYRAZOLOPYRIMIDINE MACROCYCLES AS INHIBITORS OF HUMAN IMMUNODEFICIENCY VIRUS REPLICATION
-
The disclosure generally relates to compounds of formula I, including compositions and methods for treating human immunodeficiency virus (HIV) infection. The disclosure provides novel inhibitors of HIV integrase, pharmaceutical compositions containing such compounds, and methods for using these compounds in the treatment of HIV infection.
- -
-
Page/Page column 54
(2015/09/23)
-
- Mild and selective Et2Zn-catalyzed reduction of tertiary amides under Hydrosilylation conditions
-
Diethylzinc (Et2Zn) can be used as an efficient and chemoselective catalyst for the reduction of tertiary amides under mild reaction conditions employing cost-effective polymeric silane (PMHS) as the hydride source. Crucial for the catalytic activity was the addition of a substoichiometric amount of lithium chloride to the reaction mixture. A series of amides containing different additional functional groups were reduced to their corresponding amines, and the products were isolated in good-to-excellent yields.
- Kovalenko, Oleksandr O.,Volkov, Alexey,Adolfsson, Hans
-
supporting information
p. 446 - 449
(2015/03/05)
-
- ROMP-derived oligomeric phosphates for application in facile benzylation
-
The development of new ROMP-based oligomeric benzyl phosphates (OBP n) is reported for use as soluble, stable benzylating reagents. These oligomeric reagents are readily synthesized from commercially available materials and conveniently polymerized and purified in a one-pot process, affording bench-stable, pure white, free-flowing solids on multigram scale. Utilization in benzylation reactions with a variety of nucleophiles is reported.
- Long, Toby R.,Maity, Pradip K.,Samarakoon, Thiwanka B.,Hanson, Paul R.
-
supporting information; experimental part
p. 2904 - 2907
(2010/09/30)
-
- Structure-activity relationship studies of novel 4-[2-[bis(4- fluorophenyl)methoxy]ethyl]-1-(3-phenylpropyl)piperidine analogs: Synthesis and biological evaluation at the dopamine and serotonin transporter sites
-
Several analogs of the potent dopamine (DA) transporter ligand 4-[2- [bis(4-fluorophenyl)-methoxy]ethyl]-1-(3-phenylpropyl)piperidine, 1b, were made and biologically evaluated for their binding at the DA and serotonin (5HT) transporters in rat striatal membranes. Different alkyl chain lengths and substitutions were introduced in these molecules to generate an optimum activity and selectivity for the DA transporter. In general, unsubstituted and fluoro-substituted compounds were the most active and selective for the DA transporter. The compound 4-[2(diphenylmethoxy)ethyl]-1-benzylpiperidine, 9a, showed high potency and was the most selective for the DA transporter (5HT/DA = 49) in this series of compounds. Some of these novel analogs were found to be more selective in binding at the DA transporter than the original GBR 12909 molecule, 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(3- phenylpropyl)piperidine.
- Dutta,Xu,Reith
-
p. 749 - 756
(2007/10/03)
-
- SYNTHESIS AND ANTIBACTERIAL ACTIVITY OF NEW 7-SUBSTITUTED FLUOROQUINOLONES
-
Reaction of substitued 3-carboxyquinolone derivatives IIIa, IIIb, IIIc, and IV with 4-pyridone ethylene ketal in pyridine afforded corresponding 7-substituted derivatives VIa, VIb, VIc, and VIIa, respectively.Acidic deprotecion of these compounds yielded respective oxo derivatives VId, VIe, VIf, and VIIb which were converted to their oximes If, Ig, Ih, and IIb.
- Radl, Stanislav,Kovarova, Lenka
-
p. 2406 - 2412
(2007/10/02)
-
- Synthesis of the new α- and β-adrenergic antagonist 1-[1-(2-benzodioxanylmethyl)-4-piperidyl]amino-3-(1-naphthoxy)-2- propanol
-
The synthesis and in vitro α- and β-adrenergic blocking potency of 1-[1-(2-benzodiaxanylmethyl)-4-piperidyl]amino-3-(1-naphthoxy)-2- propanol (I) are described. Thus, N-benzyl-4piperidone was protected and debenzylated to the carbamate (V), which upon alkaline hydrolysis and acylation gave benzodioxanic amide (IX). Reduction of the amide group, deprotection of the ketone function of (X), and reductive amination gave the 4-aminopiperidine (XIII), which was finally condensed with the appropriate epoxide to yield the aminopropanol (I). Compound (I) is formally derived from a combination of piperoxan (II) and propranolol (III), and was approximately 10 times less potent than each one of these drugs, as an α- and β-adrenergic blocker respectively.
- Mauleon,Antunez,Rosell
-
p. 1109 - 1117
(2007/10/02)
-