a general, simple, practical and convenient method has been described for the synthesis of anesthetic drug thiopental using thiourea in the presence of sodium ethoxide. anesthetic drug of thiopental was prepared in two stages; during the first stage, the alkylation of mthyl cyanoacetate was performed which was then to be followed by cyclization. alkylation of methyl cyanoacetate which was perfo...

One-pot Fischer indolisation indole N-alkylation enables straightforward, rapid synthesis of structurally-diverse 1,2,3-trisubstituted indoles from simple, widely-available precursors.

Alkylation of quinolin-2(1H)-one (1) and its C(6) and C(7) substituted dervatives (OMe, OBn, and Cl) with 2-bromoacetophenone or chloroacetone under basic condition (K2CO3 in DMF) gave a mixture of N1and O2alkylated products with the former one as a major product. However, alkylation of 8-methoxy-, 8-benzyloxy-, and 8-chloroquinolin-2(1H)-ones under the same reaction conditions gave exclusively...

Recently, a number of papers have emerged demonstrating copper-catalyzed alkylation reactions of electron-rich small molecules. The processes are generally thought to be related to long established atom-transfer radical reactions. However, unlike classical reactions, these new transformations lead to simple alkylation products. This short review will highlight recent advances in alkylations of ...

A boron-based catalyst was found to catalyze the straightforward alkylation of amines with readily available carboxylic acids in the presence of silane as the reducing agent. Various types of primary and secondary amines can be smoothly alkylated with good selectivity and good functional-group compatibility. This metal-free amine alkylation was successfully applied to the synthesis of three com...

An efficient, general procedure for highly chemoselective reductive mono-alkylation of ammonia with ketones is reported. Treatment of ketones with ammonia in ethanol and titanium(IV) isopropoxide, followed by in situ sodium borohydride reduction, and a straightforward workup afforded primary amines in good to excellent yields. Reductive alkylation of ammonia with aldehydes, on the other hand, a...

Citation for published version: Butts, CP, Filali, E, Lloyd-jones, GC, Norrby, P, Sale, DA & Schramm, Y 2009, 'Structure-Based Rationale for Selectivity in the Asymmetric Allylic Alkylation of Cycloalkenyl Esters Employing the Trost ‘Standard Ligand’ (TSL): Isolation, Analysis and Alkylation of the Monomeric form of the Cationic 3-Cyclohexenyl Complex [(3-c-C6H9)Pd(TSL)]+' Journal of the Americ...

The chemistry of the active site of bovine pancreatic ribonuclease has been further examined by study of the reaction of iodoacetic acid with histidine residues 12 and 119 in derivatives of the protein. In the native enzyme, the stereospecific alkylation of the two imidazole rings is a mutually exclusive, electrostatically oriented reaction leading to a 7 : 1 ratio of substitution at residues 1...

The in vivo alkylation of DNA by N-nitrosomethyl-(2-hydroxyethyl)amine (NMHEA) was examined in male and female F-344/N rats. NMHEA is a strong hepatocarcinogen in female rats when administered by gavage but a weaker hepatocarcinogen in male rats. Groups of 5 rats of each sex were treated by gavage with various doses of NMHEA dissolved in corn oil. After 4 h the animals were sacrificed and the l...

Co(II)-based metalloradical catalysis has, for the first time, been successfully applied for asymmetric intramolecular C–H alkylation of acceptor/acceptor-substituted diazo reagents. Through the design and synthesis of a new D2-symmetric chiral amidoporphyrin as the supporting ligand, the Co(II)-based metalloradical system, which operates at room temperature, is capable of 1,5-C–H alkylation of...