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US 12,281,179 B2Granted
Solution phase synthesis of β-turn peptidomimetic cyclic salts
OwnerSébastien Rocchi, Chantal Devin +2inventors
InventorsSébastien Rocchi, Chantal Devin, Wei Tian, Martin Bohlin
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Abstract
The present disclosure relates to methods of preparing and crystallizing β-turn cyclic peptidomimetic salts of formula I: where R1, R2, R3, R4, R5, R6, R7, R8, R10, X, Y and n are as defined in the specification. The present disclosure provides a more efficient route for preparing a crystalline form of a β-turn cyclic peptidomimetic compounds and salts thereof.
Claims1
A method for preparing a protected linear peptidomimetic compound of formula (4a)
- the method comprising the steps of:
- (a) providing tetrapeptide H-Glu(OtBu)-Lys(Boc)-Hser(Trt)-GlyOtBu;
- (b) reacting tetrapeptide H-Glu(OtBu)-Lys(Boc)-Hser(Trt)-GlyOtBu with 2-fluoro-5-nitro-benzoic acid (FNBA) to obtain a reaction mixture comprising the compound of formula (4a);
- and
- (c) precipitating the compound of formula (4a) in an organic solution comprising methyltetrahydrofuran (MeTHF) and methyl-t-butyl ether (MTBE) in a volume ratio of about one to one and wherein precipitating is carried out at a temperature of 20° C.
2 more elements
Dependencies are inferred from the claim text.