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US 2026/0285896 A1Published application
Process For The Purification Of 2-Methoxyestradiol From 4- Methoxyestradiol And Intermediates Of The Process
AssigneeIndustriale Chimica S.R.L.
InventorsRoberto LENNA, Claudio DELFRATE, Davide RIGAMONTI, Michele BOGHI
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Abstract
The present invention refers to the sector of the processes for the preparation of active ingredients for pharmaceutical use, and in particular to a process for the purification on industrial scale of (17β)-2-methoxy-estra-1,3,5(10)-triene-3,17-diol, also known as 2-methoxyestradiol, from (17β)-4-methoxy-estra-1,3,5(10)-triene-3,17-diol, also known as 4-methoxyestradiol; the invention also refers to intermediates of such a process.
Claims10
Process for the purification of 2-methoxyestradiol from 4-methoxyestradiol comprising the following steps:
- a) reaction of a mixture (N-3) comprising 2-methoxyestradiol and 4-methoxyestradiol with:
- a′) a carboxylic acid selected from formic acid, acetic acid and propionic acid or
- a″) the derivative of a carboxylic acid selected from an ester, an anhydride, an acyl chloride and an acyl bromide,
- obtaining:
- in case a′) a mixture N-2′ comprising the corresponding monoesters in position 17 of the steroid skeleton:
- in case a″) a mixture N-2″ comprising the corresponding diesters in positions 3 and 17 of the steroid skeleton:
- wherein X is O-alkyl or O-aryl in case of esters, OCO-alkyl in case of anhydrides, and Cl or Br in case of acyl chlorides and acyl bromides;
- b) separation by crystallization of derivative N-1′ or of derivative N-1″ from mixture N-2′ or N-2″, respectively:
- c) hydrolysis of derivative N-1′ or of derivative N-1″ to yield 2-methoxyestradiol:
6 more elements
Dependencies are inferred from the claim text.