PAN, CLARK,ZHENG, XIAOYANG,MILLER, ROBERT J.,KUTZKO, JOSEPH,ZHU, YUNXIANG,PATTERSON, DUNCAN,PEER, ANDREAS,KONOWICZ, PAUL A.,AVILA, LUIS Z.,STEFANO, JAMES E,REARDON, MICHAEL R.,HARRAHY, JOHN,ZHOU, QUN
申请号:
ES12160009
公开号:
ES2534056T3
申请日:
2009.12.11
申请国别(地区):
ES
年份:
2015
代理人:
摘要:
A method of preparing a compound having Formula VIIA: ** Formula ** wherein: R1 is selected from hydrogen, hydroxyl, an alkyl group with 1 to 4 carbons, optionally substituted, phosphate, sulfate, -OR7, a protecting group , and a saccharide; R2, R3, R4 and R5 are each independently selected from hydrogen, sulfate, hydroxyl, -OR8, a protecting group and a saccharide; R6 is selected from hydrogen, hydroxy, carboxyl, alkoxycarbonyl, amino, amide, alkylamino, aminoalkyl, aminoxy, hydrazide, hydrazine, optionally substituted alkenyl and optionally substituted C2-C6 alkyl; R7 and R8 are each independently selected from acetyl and an optionally substituted alkyl group with 1 to 4 carbons; and n is an integer from 1 to 10; which comprises: a) treating a compound having Formula VIIIA: ** Formula ** wherein: R1 to R5 are as defined above; and R9 and R10 are chosen from hydrogen and hydroxyl, so that when one of R9 and R10 is hydroxyl, the other is hydrogen; with a compound having the Formula R11R12 (Sn>; = O) to form a compound having the Formula IXA: wherein: R1 to R5 are as defined above; and R11 and R12 are each independently selected from unsubstituted alkyl, or R11 and R12, taken together, are chosen from unsubstituted alkylene; and b) treating the compound of Formula IXA, optionally in the presence of a metal halide, with a compound having the Formula R6- (CH2) n-L, wherein: R6 and n are as defined above; and L is a halogen; to form the compound of Formula VIIAUn método de preparar un compuesto que tiene la Fórmula VIIA: **Fórmula** en donde: R1 se elige de hidrógeno, hidroxilo, un grupo alquilo con 1 a 4 carbonos, opcionalmente sustituido, fosfato, sulfato, -OR7, un grupo protector, y un sacárido; R2, R3, R4 y R5 se eligen, cada uno independientemente, de hidrógeno, sulfato, hidroxilo, -OR8, un grupo protector y un sacárido; R6 se elige de hidrógeno, hidroxilo, carboxilo, alcoxicarbonilo, amino, amida, alquilamino, aminoalquilo, aminoxi, hidrazida, hidrazina, alqueni