A new approach to the synthesis of cilastatin, an inhibitor of renal dipeptidase

Autor:	L. N. Kalgorodova, G. I. Nikishin, Maxim G. Vinogradov, A. V. Ignatenko, E. K. Starostin, G. V. Chel'tsova-Bebutova, L. S. Gorshkova, E. A. Shapiro
Rok vydání:	1995
Předmět:	Imipenem Cilastatin Chemistry Cyclopropanation Halogenation General Chemistry Chloride Combinatorial chemistry Cycloheptanone chemistry.chemical_compound Reagent medicine Amination medicine.drug
Zdroj:	Russian Chemical Bulletin. 44:167-171
ISSN:	1573-9171 1066-5285
DOI:	10.1007/bf00696982
Popis:	A convenient preparative synthesis of cilastatin, an inhibitor of renal dipeptidase used in drugs with the antibiotic imipenem, has been elaborated. The key intermediate in this synthesis is 2-amino-7-chloroheptanoic acid prepared by oxidative cleavage of cycloheptanone followed by bromination of 7-chloroheptanoyl chloride with subsequent amination of the 2-bromo-7-chloroheptanoic acid thus formed. All of the stages of the new synthesis are easily performed, as is the isolation of the intermediate products, and they do not require any organometallic reagents.
Databáze:	OpenAIRE
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