Patent · US Expired

Process and intermediates for the production of 7-substituted antiestrogens

US7947667B2 · kind B2 · utility

0Cited by
9References
5Claims
0Family size

Assignee

Inventors

Key dates

Filing dateOct 9, 2001
Grant dateMay 24, 2011
Priority date
Expiry dateOct 9, 2021

Classification

  • Technology area (CPC Y)Emerging Cross-Sectional Technologies
  • CPC primaryY02P20/55
  • WIPO fieldOrganic fine chemistry
  • WIPO sectorChemistry

Abstract

A process for preparing an intermediate compound of formula (II)where X is as defined in the specification, R1 is haloalkyl, alkyl, alkenyl, cycloalkyl, carboxyalkyl, alkoxycarbonylalkyl, aryl or arylalkyl;R2, R3, R4 and R5 are organic groups as defined in the specification, which process comprises aromatisation of a compound of formula (III)where R1, R2, R3, n, X and R5 are as defined in relation to formula (II) and R4′ is a group R4 or a precursor group thereof, and thereafter if necessary or desired, carrying out one or more of the following steps: (i) removing any hydroxy-protecting groups R; (ii) converting a precursor group R4′ to a group R4, or where R4′ is a group R4, converting it to a different such group.Compounds obtained are useful intermediates for example in the preparation of fulvestrant. Novel intermediates are also claimed.

Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.