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process for the preparation of a compound of formula (i) and process for the preparation of estetrol
专利权人:
ESTETRA S.A.;ESTETRA S.P.R.L.
发明人:
JEAN-CLAUDE PASCAL
申请号:
BR112013030833
公开号:
BR112013030833B1
申请日:
2012.06.01
申请国别(地区):
BR
年份:
2019
代理人:
摘要:
"Process for the preparation of a compound of formula (i) and process for the preparation of estetrol and estetrol" the present invention relates to a process for the preparation of a compound of formula (i) comprising the steps of a ) reacting a compound of formula (ii) with a silylating or acylating agent to produce the compound of formula (iii), wherein p1 is a protecting group selected from r2-si-r3r4 or r1co-, r1 is a group selected from alkyl C 1-6 or C 3-6 cycloalkyl, wherein each group is optionally substituted by one or more substituents independently selected from fluoro or C 1-4 alkyl; R 2, R 3 and R 4 are each independently a group selected from C 1-6 alkyl or phenyl, wherein each group is optionally substituted by one or more substituents independently selected from fluoro or C 1-4 alkyl; b) halogenating or sulfinylating the compound of formula (iii) to produce a compound of formula (iv); wherein x is halo, or -o-so-r5 and r5 is a group selected from heteroaryl or C6-10 aryl, each group being optionally substituted by one or more substituents independently selected from chlorine or C1-4 alkyl; c) dehalogenating or desulfinylating the compound of formula (iv) to produce the compound of formula (v); and d) reacting the compound of formula (v) with a reducing agent to produce the compound of formula (i).“processo para a preparação de um composto de fórmula (i) e, processo para a preparação de estetrol e estetrol” a presente invenção refere-se a um processo para a preparação de um composto de fórmula (i) que compreende as etapas de a) reagir um composto de fórmula (ii) com um agente sililante ou acilante para produzir o composto de fórmula (iii), em que p1 é um grupo protetor selecionado dentre r2-si-r3r4 ou r1co-, r1 é um grupo selecionado dentre alquila c1-6 ou cicloalquila c3-6, em que cada grupo é opcionalmente substituído por um ou mais substituintes independentemente selecionados dentre fluoro ou alquila c1- 4; r2, r3 e r4 são cada um independentement
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