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Process for the preparation of ibodutant (MEN15596) and related intermediates
专利权人:
Fabrizio Bonaccorsi;Valentina Fedi;Danilo Giannotti
发明人:
Fabrizio Bonaccorsi,Valentina Fedi,Danilo Giannotti
申请号:
US13321501
公开号:
US08431684B2
申请日:
2010.05.11
申请国别(地区):
US
年份:
2013
代理人:
摘要:
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).
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