Method for the preparation of cyclopeptides
AssigneeDSM Sinochem Pharmaceuticals Netherlands B.V.
InventorsRobertus Mattheus De Pater, Dhiredj Chandre Jagesar, Thomas Van Der Does
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Abstract
The present invention relates to a method for preparing cyclopeptides by means of protection with a substituted boronic acid. The present invention also discloses novel boronate esters of cyclopeptides of general formula (8).
Claims14
Method for the preparation of a first cyclopeptide comprising a vicinal diol from a second cyclopeptide comprising a vicinal diol characterized in that said vicinal diol in said second cyclopeptide is protected by reaction with a substituted boronic acid R5—B(OH)2 that is not phenylboronic acid or naphthylboronic acid.
A compound of the general formula ()
- wherein R1 is C(O)R2 wherein R2 is C9-C21 alkyl, C9-C21 alkenyl, C1-C10 alkoxyphenyl, C1-C10 alkoxynaphthyl or C1-C10 alkoxyterphenyl, wherein R4 is OH or —SR3 wherein R3 is benzimidazol-2-yl, benzothiazol-2-yl, 1-methylimidazol-2-yl, 4-methoxyphenyl or phenyl, wherein R5 is cyclohexyl, substituted cyclohexyl or substituted phenyl and wherein X is O or H,H.
Use of cyclohexylboronic acid or 4-tert-butylphenylboronic acid in the preparation of a cyclopeptide bearing a vicinal diol.
Dependencies are inferred from the claim text.