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Process for the production of estetrol intermediaries
专利权人:
Estetra S.P.R.L.
发明人:
PASCAL, Jean-Claude
申请号:
ES12729053
公开号:
ES2600703T3
申请日:
2012.06.01
申请国别(地区):
ES
年份:
2017
代理人:
摘要:
Process for the preparation of a compound of the formula (I) ** Formula ** comprising the steps of a) reacting a compound of the formula (II), with a silylating agent or an acylating agent to produce a compound of the formula (III), wherein P1 is a protecting group that is selected from R2-Si-R3R4 or R1CO-, R1 is a group selected from C1-6alkyl or C3-6cycloalkyl, each group being optionally substituted by one or more substituents independently selected from fluorine or C1-4alkyl; R2, R3 and R4 are each independently a group selected from C1-6alkyl or phenyl, each group being optionally substituted by one or more substituents independently selected from fluorine or C1-4alkyl; ** Formula ** b) halogenation or sulfinylation of the compound of formula (III) to produce a compound of formula (IV); wherein X is halo or -SO-R5 and R5 is a group selected from C6-10aryl or heteroaryl, each group being optionally substituted by one or more substituents independently selected from chlorine or C1-4alkyl; ** Formula ** c ) dehalogenation or desulfinylation of the compound of formula (IV) to produce the compound of formula (V); and ** Formula ** d) reacting the compound of formula (V) with a reducing agent to produce a compound of formula (I), and where C6-10aryl is intended to also include partially hydrogenated derivatives.Proceso para la preparación de un compuesto de la fórmula (I)**Fórmula** que comprende las etapas de a) hacer reaccionar un compuesto de la fórmula (II), con un agente sililante o un agente acilante para producir un compuesto de la fórmula (III), en donde P1 es un grupo protector que se selecciona de R2-Si- R3R4 o R1CO-, R1 es un grupo seleccionado de C1-6alquilo o C3-6cicloalquilo, siendo cada grupo opcionalmente sustituido por uno o más sustituyentes independientemente seleccionados de flúor o C1- 4alquilo; R2,R3 y R4 son cada uno independientemente un grupo seleccionado de C1-6alquilo o fenilo, siendo cada grupo opcionalmente sustituido por uno o más sustit
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