Process for the preparation of ibodutant (MEN15596) and related intermediates
US8431684B2 · kind B2 · utility
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7Claims
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Key dates
| Filing date | May 11, 2010 |
| Grant date | Apr 30, 2013 |
| Priority date | — |
| Expiry date | May 11, 2030 |
Classification
- Technology area (CPC A)Human Necessities
- CPC primaryA61P43/00
- WIPO fieldPharmaceuticals
- WIPO sectorChemistry
Abstract
This invention relates to a novel process for synthesizing the product ibodutant shown in the figure below, consisting of a small number of high-yield steps involving reagents and solvents with low environmental impact, characterized by the coupling of two portions, compounds (3) and (4), one of which (3) is synthesized by coupling of 6-methyl-2-benzo[b]thiophenecarboxylic acid (1) with 1-amino-alpha-alpha-cyclopentan carboxylic acid and subsequent cyclization with oxazolone, while the other, compound (4), is obtained from suitable highly selective functionalizations of 4-aminomethylpiperidine (2).
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.