C07C309/77

Non-chromatographic purification of macrocyclic peptides by a resin catch and release

The disclosure is directed to compounds and methods for preparing purified macrocyclic peptide using “catch-release” methods. These methods comprise reacting a free amino group of a resin-bound linear peptide with an azide- or alkyne-functionalized cap to form a resin-bound capped linear peptide having an azide- or alkyne-functionalized cap; cleaving the capped linear peptide from the resin to form a free capped linear peptide having an azide- or alkyne-functionalized cap; reacting the free capped linear peptide having an azide-functionalized cap with an alkyne-functionalized catch resin, or reacting the free capped linear peptide having an akynyl-functionalized cap with an azide functionalized catch resin, to form a catch-resin bound capped linear peptide; reacting the catch-resin bound capped linear peptide under conditions sufficient to effect macrocyclization of the linear peptide and release of the macrocyclic peptide from the catch resin.

Non-chromatographic purification of macrocyclic peptides by a resin catch and release

The disclosure is directed to compounds and methods for preparing purified macrocyclic peptide using “catch-release” methods. These methods comprise reacting a free amino group of a resin-bound linear peptide with an azide- or alkyne-functionalized cap to form a resin-bound capped linear peptide having an azide- or alkyne-functionalized cap; cleaving the capped linear peptide from the resin to form a free capped linear peptide having an azide- or alkyne-functionalized cap; reacting the free capped linear peptide having an azide-functionalized cap with an alkyne-functionalized catch resin, or reacting the free capped linear peptide having an akynyl-functionalized cap with an azide functionalized catch resin, to form a catch-resin bound capped linear peptide; reacting the catch-resin bound capped linear peptide under conditions sufficient to effect macrocyclization of the linear peptide and release of the macrocyclic peptide from the catch resin.

NON-CHROMATOGRAPHIC PURIFICATION OF MACROCYCLIC PEPTIDES BY A RESIN CATCH AND RELEASE

The disclosure is directed to compounds and methods for preparing purified macrocyclic peptide using catch-release methods. These methods comprise reacting a free amino group of a resin-bound linear peptide with an azide- or alkyne-functionalized cap to form a resin-bound capped linear peptide having an azide- or alkyne-functionalized cap; cleaving said capped linear peptide from the resin to form a free capped linear peptide having an azide- or alkyne-functionalized cap; reacting the free capped linear peptide having an azide-functionalized cap with an alkyne-functionalized catch resin, or reacting the free capped linear peptide having an akynyl-functionalized cap with an azide functionalized catch resin, to form a catch-resin bound capped linear peptide; reacting the catch-resin bound capped linear peptide under conditions sufficient to effect macrocyclization of the linear peptide and release of the macrocyclic peptide from the catch resin.

NON-CHROMATOGRAPHIC PURIFICATION OF MACROCYCLIC PEPTIDES BY A RESIN CATCH AND RELEASE

The disclosure is directed to compounds and methods for preparing purified macrocyclic peptide using catch-release methods. These methods comprise reacting a free amino group of a resin-bound linear peptide with an azide- or alkyne-functionalized cap to form a resin-bound capped linear peptide having an azide- or alkyne-functionalized cap; cleaving said capped linear peptide from the resin to form a free capped linear peptide having an azide- or alkyne-functionalized cap; reacting the free capped linear peptide having an azide-functionalized cap with an alkyne-functionalized catch resin, or reacting the free capped linear peptide having an akynyl-functionalized cap with an azide functionalized catch resin, to form a catch-resin bound capped linear peptide; reacting the catch-resin bound capped linear peptide under conditions sufficient to effect macrocyclization of the linear peptide and release of the macrocyclic peptide from the catch resin.

Preparation of phenyl compounds

The invention relates to a method for preparing a compound comprising two phenyl groups by reacting a bisfuranic compound with a dienophile; and to such compounds.

Preparation of phenyl compounds

The invention relates to a method for preparing a compound comprising two phenyl groups by reacting a bisfuranic compound with a dienophile; and to such compounds.

RADIOACTIVE FLUORINE-LABELED PRECURSOR COMPOUND, AND METHOD FOR PRODUCING RADIOACTIVE FLUORINE-LABELED COMPOUND USING SAME

There is provided a labeling precursor compound represented by the general formula (2):

##STR00001##

wherein S represents a substrate, L represents a straight alkyl group having 1 to 6 carbon atoms which may contain an ether group, R.sup.1 and R.sup.2 each independently represent a straight or branched alkyl group having 1 to 30 carbon atoms, or a substituted or unsubstituted monocyclic or condensed polycyclic aryl group, R.sup.3 each independently represent an alkyl group having 1 to 4 carbon atoms or an alkoxy group having 1 to 4 carbon atoms, and p represents an integer of 0 to 4.

RADIOACTIVE FLUORINE-LABELED PRECURSOR COMPOUND, AND METHOD FOR PRODUCING RADIOACTIVE FLUORINE-LABELED COMPOUND USING SAME

There is provided a labeling precursor compound represented by the general formula (2):

##STR00001##

wherein S represents a substrate, L represents a straight alkyl group having 1 to 6 carbon atoms which may contain an ether group, R.sup.1 and R.sup.2 each independently represent a straight or branched alkyl group having 1 to 30 carbon atoms, or a substituted or unsubstituted monocyclic or condensed polycyclic aryl group, R.sup.3 each independently represent an alkyl group having 1 to 4 carbon atoms or an alkoxy group having 1 to 4 carbon atoms, and p represents an integer of 0 to 4.

NON-CHROMATOGRAPHIC PURIFICATION OF MACROCYCLIC PEPTIDES BY A RESIN CATCH AND RELEASE

The disclosure is directed to the synthesis and improved methods for purifying macrocyclic peptides produced by solid phase peptide synthesis.

NON-CHROMATOGRAPHIC PURIFICATION OF MACROCYCLIC PEPTIDES BY A RESIN CATCH AND RELEASE

The disclosure is directed to the synthesis and improved methods for purifying macrocyclic peptides produced by solid phase peptide synthesis.