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Reductive Alkylation (reductive + alkylation)

Distribution by Scientific Domains
Chemistry75%

Selected Abstracts

Direct, One-pot Sequential Reductive Alkylation of Lactams/Amides with Grignard and Organolithium Reagents through Lactam/Amide Activation,

ANGEWANDTE CHEMIE, Issue 17 2010
Kai-Jiong Xiao
Erst R1, dann R2: Ein effizienter und universeller Eintopfprozess für die reduktive doppelte Alkylierung von Lactamen oder Amiden mit Grignard- und Organolithiumreagentien wurde entwickelt (siehe Schema; DTBMP=2,6-Di- tert -butyl-4-methylpyridin, Tf=Trifluormethansulfonyl). [source]

Catalytic Reductive Alkylation of Secondary Amine with Aldehyde and Silane by an Iridium Compound.

CHEMINFORM, Issue 32 2005
Tomoya Mizuta
Abstract For Abstract see ChemInform Abstract in Full Text. [source]

Reductive Alkylation of Perfluorocarboxylic Acid Esters with CCl3F or CCl4 and Synthesis of Higher Linear Perfluoroketones.

CHEMINFORM, Issue 16 2005
Yu. V. Zeifman
No abstract is available for this article. [source]

Reductive Alkylation of ,-Alkoxy Aziridines: New Route to Substituted Allylic Amines.

CHEMINFORM, Issue 16 2005
Clare M. Rosser
Abstract For Abstract see ChemInform Abstract in Full Text. [source]

Reductive Alkylation of Thioureas: A Highly Practical Synthesis of Unsymmetrical N,N,-Disubstituted Thioureas.

CHEMINFORM, Issue 5 2005
Lech Ciszewski
Abstract For Abstract see ChemInform Abstract in Full Text. [source]

Synthesis, asymmetric aldol reactions, and x-ray crystallography of some oxadiazinanone derivatives

JOURNAL OF HETEROCYCLIC CHEMISTRY, Issue 5 2008
Shawn R. Hitchcock
A series of N4 -substituted oxadiazinanones have been synthesized from (1R,2S)-norephedrine by a process of either reductive alkylation or arylation, N -nitrosation, reduction and cyclization. These derivatives (R = -CH2Ph, -CH2C(CH3)3, - cyclo -C6H11, -C6H5) have been acylated with propanoyl chloride and employed in the asymmetric Aldol reaction. The observed diastereoselectivities for the formation of the "non-Evans" syn-adduct ranged from 88:12 to 99:1. The hydrolysis of the Aldol adducts varied with the nature of the nitrogen substituent. [source]

Pharmacokinetic characterization of 14C-vascular endothelial growth factor controlled release microspheres using a rat model

JOURNAL OF PHARMACY AND PHARMACOLOGY: AN INTERNATI ONAL JOURNAL OF PHARMACEUTICAL SCIENCE, Issue 7 2002
Tae-Kyoung Kim
The objectives of this study were to characterize the pharmacokinetics of vascular endothelial growth factor (VEGF) in poly(lactic-co-glycolic) acid (PLGA) microspheres using a rat model, and to develop a pharmacokinetic model for this controlled release formulation. 14C-VEGF was encapsulated using a solid-in-oil-in-water emulsification method. The microspheres were administered subcutaneously to rats and the pharmacokinetic parameters were compared with those of protein solutions. Intravenous administration of protein solutions resulted in short half-lives and subcutaneous administration resulted in rapid clearance from the subcutaneous tissue, with high plasma concentrations as expressed by rapid absorption and elimination. The subcutaneous administration of the VEGF microspheres produced low plasma concentrations and high subcutaneous concentrations over a period of 7 weeks. The area under the curve (AUC), the time required to achieve the maximum concentration (tmax), the maximum concentration (Cmax) in blood samples and the elimination rate constant (kel) values at the subcutaneous tissue site were selected to compare the pharmacokinetic characterization of VEGF microspheres with that of protein solutions. The in-vivo release profiles of the proteins were slower than the in-vitro release profiles and they followed the same trend as the in-vitro and in-vivo PLGA degradation rates. The PLGA microsphere degradation was the determinant step for VEGF release from the microspheres and its absorption at the subcutaneous site. Microspheres appear to be an attractive system for the localized rate-controlled delivery of VEGF. 14C-Methylation via reductive alkylation of VEGF did not affect its mitogenic activity, however approximately 25% activity was lost following release from PLGA microspheres. This loss of activity may be due to degradation in an acidic environment as a result of PLGA degradation. [source]

Improved Anti-Inflammatory Properties for Naproxen with Cyclodextrin-Grafted Polysaccharides,

MACROMOLECULAR BIOSCIENCE, Issue 7 2006
Héctor L. Ramírez
Abstract Summary: Mannan and carboxymethylcellulose, previously activated by periodate oxidation, were grafted with mono-6-butylenediamino-6-deoxy- , -cyclodextrin derivatives by reductive alkylation in the presence of sodium borohydride. The formation of supramolecular complexes between these polymers and Naproxen was confirmed by fluorescence spectroscopy. The solubility of the drug was 3.8,4.6 fold increased in the presence of the cyclodextrin-grafted polysaccharides. The in vivo anti-inflammatory property of Naproxen was 1.7 times higher after supramolecular association with , -cyclodextrin-branched mannan. [source]