Improvement in the method for the preparation of N-(3,4-dimethoxyphenylethyl)-3′,4′-dimethoxyphenylacetamide
The synthesis of I was first described in 1909 [i]. At present several methods are known for the preparation of this compound, starting from 3,4-dimethoxyphenylethylamine (If) and 3,4-dimethoxyphenylacetic acid (III) or its acid chloride (IV) [2-4]. The use of IV makes it possible to obtain I in a yield of up to 95% [5, 6], but this method cannot be used industrially because of considerable complications of the industrial process.
Practical preparation of coralyne chloride.
Abstract Coralyne chloride was prepared by a convenient process which can be adapted to large-scale synthesis of this antileukemic alkaloid.
Highly enantio- and diastereoselective synthesis of β-methyl-γ-monofluoromethyl-substituted alcohols.
Enanatiopure β-methyl-γ-monofluoromethyl alcohols were prepared from the allylic alkylation between fluorobis(phenylsulfonyl)methane with Morita-Baylis-Hillman carbonates. The reaction was catalyzed by using the Cinchona alkaloid derivative, (DHQD)(2)AQN. The origin of the stereoselectivity was verified by DFT methods. Calculated geometries and relative energies of various transition states strongly support the observed stereoselectivity.