Abstract:
Disclosed herein is a process for the preparation of erythromycin derivatives, or pharmaceutically acceptable salts thereof, which contain an optionally substituted propargyl group at the 6-O-position.
Abstract:
Disclosed herein is a process for the preparation of erythromycin derivative s, or pharmaceutically acceptable salts thereof, which contain an optionally substituted propargyl group at the 6-O-position.
Abstract:
The invention relates to a process for preparing carbonate and carbamate compounds, which are important intermediates in the synthesis of 6-O-substituted macrolide antibiotics. The process employs metal-catalyzed coupling reactions to provide a carbonate or carbamate of formula (I) or a substrate that can be reduced to obtain the same. €ƒ€ƒ€ƒ€ƒ€ƒ€ƒ€ƒ€ƒR 1 -CH=CHCH 2 OC(O)-X-R 2 €ƒ€ƒ€ƒ€ƒ€ƒ(I)
Abstract:
Un procedimiento de preparación de un compuesto de fórmulaR1-CH>=CHCH2OC(O)-X-R2 (I),dondeR1 es quinolilo eventualmente substituido con uno o más de:(i) alquilo,(ii) alcoxi,(iii) arilo,(iv) nitro y(v) halo;R2 es alquilo C1-C10;X es -O- o -NR3; yR3 es hidrógeno, alquilo C1-C6 o arilo; o R2 y R3, tomados conjuntamente, forman un anillo aromático o noaromático, que comprende las etapas de:(a) preparación de un intermediario seleccionado entre:(i) R1-CºCCH2OR4, donde R4 es hidrógeno o un grupo hidroxi-protector;(ii) R1-CºC-CH2-OC(O)-X-R2;(b) reducción o desprotección de un intermediario obtenido en la etapa (a); y(c) copulación eventual del compuesto obtenido en la etapa (b) con un reactivo acilante.
Abstract:
Disclosed herein is a process for the preparation of erythromycin derivative s, or pharmaceutically acceptable salts thereof, which contain an optionally substituted propargyl group at the 6-O- position.