The process of obtaining butirolactonas derivatives; derivatives of butirolactonas obtained and applications thereof in pharmaceutical formulations

摘要

"The process of obtaining derivatives of butirolactonas". Butirolactonas derivatives obtained and applications thereof in pharmaceutical formulations.There are several derivatives of butirolactonas in only three synthetic steps.The optically active derivatives are obtained by the asymmetric catalytic hydrogenation in liquid phase, of methanol or ethanol under hydrogen atmosphere.In the presence of homogeneous chiral catalyst based on rhodium acid 4 - (aminofenil) - 3metoxicarbonil - 3 - butenu00f3ico and acid 4 - (nitrophenyl) - 3 - methoxycarbonyl - 3 - butenu00f3ico,Followed by reduction quimiosseletiva of grouping ester and lactonizau00e7u00e3o in acid medium.The racu00eamicos derivatives can be obtained in a similar way using heterogeneous base catalyst of palladium supported on activated carbon.The unsaturated acids, 4 - (methoxycarbonyl aminofenil) - 3 - 3 - butenu00f3ico and 4 - (nitrophenyl) - 3 - methoxycarbonyl - 3 - butenu00f3ico, in turn,Are obtained with a good yield by condensation of dimetile succinate with 1 -, 2 - or 3 - aminobenzaldeu00eddo or with 1 -, 2 - or 3 - nitrobenzaldeu00eddo,Using as a basis the metu00f3xido sodium dissolved in anhydrous methanol, or the etu00f3xido sodium dissolved in anhydrous ethanol, or, preferably,The T - no sodium or potassium dissolved in T - butanol, anhydrous.