Patent classifications
C07C33/16
FUSED CYCLOOCTYNE COMPOUNDS AND THEIR USE IN METAL-FREE CLICK REACTIONS
The invention relates to fused cyclooctyne compounds, and to a method for their preparation. The invention also relates to a conjugate wherein a fused cyclooctyne compound according to the invention is conjugated to a label, and to the use of these conjugates in bioorthogonal labeling, imaging and/or modification, such as for example surface modification, of a target molecule. The invention further relates to a method for the modification of a target molecule, wherein a conjugate according to the invention is reacted with a compound comprising a 1,3-dipole or a 1,3-(hetero)diene.
FUSED CYCLOOCTYNE COMPOUNDS AND THEIR USE IN METAL-FREE CLICK REACTIONS
The invention relates to fused cyclooctyne compounds, and to a method for their preparation. The invention also relates to a conjugate wherein a fused cyclooctyne compound according to the invention is conjugated to a label, and to the use of these conjugates in bioorthogonal labeling, imaging and/or modification, such as for example surface modification, of a target molecule. The invention further relates to a method for the modification of a target molecule, wherein a conjugate according to the invention is reacted with a compound comprising a 1,3-dipole or a 1,3-(hetero)diene.
FUSED CYCLOOCTYNE COMPOUNDS AND THEIR USE IN METAL-FREE CLICK REACTIONS
The invention relates to fused cyclooctyne compounds, and to a method for their preparation. The invention also relates to a conjugate wherein a fused cyclooctyne compound according to the invention is conjugated to a label, and to the use of these conjugates in bioorthogonal labeling, imaging and/or modification, such as for example surface modification, of a target molecule. The invention further relates to a method for the modification of a target molecule, wherein a conjugate according to the invention is reacted with a compound comprising a 1,3-dipole or a 1,3-(hetero)diene.
Cleavable tetrazine used in bio-orthogonal drug activation
Disclosed is an advancement in provoked chemical cleavage. Thereby the invention provides the use of a diene as a chemically cleavable group attached to a Construct, and the use of a dienophile to provoke the release of the Construct by allowing the diene to react with a dienophile capable of undergoing an inverse electron demand Diels Alder reaction with the diene. The invention includes a kit for releasing a Construct C.sup.A bound to a Trigger T.sup.R, the kit having a tetrazine and a dienophile, wherein the Trigger is the tetrazine. The invention also includes the use of the formation of a pyridazine by reacting a tetrazine having a Construct C.sup.A bound thereto and a dienophile, as a chemical tool for the release, in a chemical, biological or physiological environment, of the Construct.
SELECTIVE HYDROGENATION OF ALKYNOLS TO ALKENOLS IN THE PRESENCE OF A PHOSPHORUS COMPOUND
The present invention relates to a process of hydrogenating an alkynol selectively to an alkenol by hydrogen using a hydrogenation catalyst which is palladium supported on a carrier in the presence of an additive which is an organic phosphorus compound bearing either a phosphine or a phosphine oxide group and with the proviso that if the additive bears a phosphino group that the additive bears two or more phosphino groups.
SELECTIVE HYDROGENATION OF ALKYNOLS TO ALKENOLS IN THE PRESENCE OF A PHOSPHORUS COMPOUND
The present invention relates to a process of hydrogenating an alkynol selectively to an alkenol by hydrogen using a hydrogenation catalyst which is palladium supported on a carrier in the presence of an additive which is an organic phosphorus compound bearing either a phosphine or a phosphine oxide group and with the proviso that if the additive bears a phosphino group that the additive bears two or more phosphino groups.
Fused cyclooctyne compounds and their use in metal-free click reactions
The invention relates to fused cyclooctyne compounds, and to a method for their preparation. The invention also relates to a conjugate wherein a fused cyclooctyne compound according to the invention is conjugated to a label, and to the use of these conjugates in bioorthogonal labeling, imaging and/or modification, such as for example surface modification, of a target molecule. The invention further relates to a method for the modification of a target molecule, wherein a conjugate according to the invention is reacted with a compound comprising a 1,3-dipole or a 1,3-(hetero)diene.
Fused cyclooctyne compounds and their use in metal-free click reactions
The invention relates to fused cyclooctyne compounds, and to a method for their preparation. The invention also relates to a conjugate wherein a fused cyclooctyne compound according to the invention is conjugated to a label, and to the use of these conjugates in bioorthogonal labeling, imaging and/or modification, such as for example surface modification, of a target molecule. The invention further relates to a method for the modification of a target molecule, wherein a conjugate according to the invention is reacted with a compound comprising a 1,3-dipole or a 1,3-(hetero)diene.
Fused cyclooctyne compounds and their use in metal-free click reactions
The invention relates to fused cyclooctyne compounds, and to a method for their preparation. The invention also relates to a conjugate wherein a fused cyclooctyne compound according to the invention is conjugated to a label, and to the use of these conjugates in bioorthogonal labeling, imaging and/or modification, such as for example surface modification, of a target molecule. The invention further relates to a method for the modification of a target molecule, wherein a conjugate according to the invention is reacted with a compound comprising a 1,3-dipole or a 1,3-(hetero)diene.
SELECTIVE HYDROGENATION OF ALKYNES TO ALKENES IN THE PRESENCE OF A PHOSPHORUS COMPOUND AND AN ORGANIC SULPHUR COMPOUND
The present invention relates to a process of hydrogenating an alkyne selectively to an alkene by hydrogen using a hydrogenation catalyst which is palladium supported on a carrier in the presence of an additive mixture of an organic phosphorus compound (AP) and an organic sulphur compound (AS).