Abstract:
PROBLEM TO BE SOLVED: To provide a method for preparing quinoline-substituted carbonate and carbamate compounds which are important intermediates in the synthesis of a 6-O-substituted macrolide antibiotic material. SOLUTION: The carbonate or carbamate derivative expressed by the formula: R 1 -CH=CHCH 2 OC(O)-X-R 2 (I) is obtained by coupling a haloquinoline with propargyl alcohol in the presence of a base and a palladium-based catalyst to form an alkynol, reducing it to make an alkenol and then reacting it with an acylation reagent. COPYRIGHT: (C)2011,JPO&INPIT
Abstract:
Disclosed is an improved and efficient process for N-desmethylating the 3'-amino nitrogen of erythromycins and for converting the 3'-N-desmethylated erythromycins into 3'-N-substituted derivatives of 8,9-anhydro-erythromycin 6,9-hemiketals.
Abstract:
Disclosed is an improved and efficient process for N-desmethylating the 3'-amino nitrogen of erythromycins and for converting the 3'-N-desmethylated erythromycins into 3'-N-substituted derivatives of 8,9-anhydro-erythromycin 6,9-hemiketals.
Abstract:
The invention relates to a process for preparing quinoline-substituted 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 (II) or substrate that can be reduced to obtain the same.
Abstract:
Disclosed is an improved and efficient process for N-desmethylating the 3'-amino nitrogen of erythromycins and for converting the 3'-N-desmethylated erythromycins into 3'-N-substituted derivatives of 8,9-anhydro-erythromycin 6,9-hemiketals.
Abstract:
Ηεφεύρεσηαφοράσεμιαμέθοδογιαπαρασκευήκινολινο-υποκατεστημένωνενώσεωνανθρακικούκαικαρβαμικού, οιοποίεςείναισημαντικάενδιάμεσαστηνσύνθεσητωναντιβιοτικών 6-O-υποκατεστημένουμακρολιδίου. Ημέθοδοςχρησιμοποιείτιςκαταλυόμενεςαπόμέταλλοαντιδράσειςσύζευξηςγιαναπαρέχειανθρακικόή καρβαμικότουτύπου (Ι) ή (II) ήυπόστρωμαπουμπορείναανάγεταιγιαναληφθούναυτά.
Abstract:
The invention relates to a process for preparing quinoline-substituted 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 (II) or a substrate that can be reduced to obtain the same.
Abstract:
Un proceso para preparar un compuesto representado por la fórmula: **(Fórmula)** y sales del mismo farmacéuticamente admisibles, en donde Rp es hidrógeno o grupo protector de hidroxi; R1 es, independientemente, hidrógeno o hidroxi en cada acontecimiento; y R2 es un radical hidrocarburo saturado C1-C8 de cadena lineal o ramificada; el método comprendiendo las etapas de: (a) tratar un compuesto representado por la fórmula: con un grupo protector de hidroxi y cloroformiato de 1-cloroetilo para proporcionar el compuesto de fórmula: **(Fórmula)**.
Abstract:
The invention relates to a process for preparing quinoline-substituted carbonate and carbamate compounds, which are important intermediates in the synthesis of 6-O-substituted marcolide antibiotics. The process employs metal-catalyzed coupling reactions to provide a carbonate or carbamate of formula (I) or (II) or substrate that can be reduced to obtain the same.