- CLEAVABLE TETRAZINE USED IN BIO-ORTHOGONAL DRUG ACTIVATION
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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 CA bound to a Trigger TR, the kit comprising 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 comprising a Construct CA bound thereto and a dienophile, as a chemical tool for the release, in a chemical, biological or physiological environment, of said Construct.
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Page/Page column 143-144; 146
(2018/02/03)
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- Formation of 4-Hydroxy-3-(α-hydroxybenzyl)-4-phenyl-2-pyrazolin-5-one from the Interaction of 3,6-Bis-(α-hydroxybenzyl)-s-tetrazine with Potassium Hydroxide in Methanol
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4-Hydroxy-3-(α-hydroxybenzyl)-4-phenyl-2-pyrazolin-5-one has been obtained from the reaction of methanolic potassium hydroxide with 3,6-bis-(α-hydroxybenzyl)-s-tetrazine and its structure proved by an alternative synthetic route.The mechanism of the rearr
- Hunter, Daniel,Neilson, Douglas G.
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p. 1371 - 1374
(2007/10/02)
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