Yield:115699-74-6 77%

Reaction Conditions:

with triethylamine in chloroform at 0 - 5; for 12 h;Inert atmosphere;

Steps:

1.2 Generalmethod for the synthesis of intermediaries (16-29)

General procedure: To a solution of theappropriate amine (31-44, 10 mmol) and triethylamine (10 mmol) in anhydrous chloroform was added dropwisechloroacetylcloride (30, 12 mmol) at0-5 °C and the mixture was stirred for 12 h at the same temperature under N₂.Then the solvent was removed under vacuum, and the residue dissolved in ethylacetate was once washed with water. The organic phase was stirred with 10%activated charcoal for 30 min and filtered through a neutral alumina bed.Finally, the solvent was distilled under vacuum. It is worth mentioning thatall the products obtained decompose rapidly, therefore they were used immediatelyin the next reaction.

References:

Velázquez-López, José Miguel;Hernández-Campos, Alicia;Yépez-Mulia, Lilián;Téllez-Valencia, Alfredo;Flores-Carrillo, Paulina;Nieto-Meneses, Rocío;Castillo, Rafael [Bioorganic and Medicinal Chemistry Letters,2016,vol. 26,# 17,p. 4377 - 4381] Location in patent:supporting information