Perseptive Biosystems Inc.

Nanda D Sinha

Jonathan N Kremsky

Richard P Hodge

The disclosed invention is drawn to pyrazolinone derivatives, and methods of use thereof, for non-radioactive labeling of amine-functionalized molecules, especially biomolecules such as DNA, RNA, PNA, oligomers, carbohydrates, amino acids and peptides. Carboxyl-containing reporter groups such as biotin and fluorescein may be activated for nucleophilic addition to a primary or secondary amine moiety. Representative compounds of the invention include Dimethoxytritylbiotin-XPP, biotin-XPP, and fluorescein-XPP.

Activated esters of 1-phenylpyrazolin-5-one for labeling

Method for production of 2'-O-derivatized uridine and cytosine RNA synthons comprising derivatizing the 2'-hydroxyl group of a partially protected cytosine ribonucleoside to preferentially produce a partially protected 2'-O-derivatized nucleoside, which is then either (1) reacted at the 3'-hydroxyl group to produce a 2'-O-derivatized cytosine RNA synthon, or (2) reacted with a hydroxide source to produce a uridine nucleobase by deamination, thereby producing a partially protected 2'-O-derivatized uridine ribonucleoside which can be reacted at its 3'-hydroxyl group to produce a uridine RNA synthon.

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Acton, MA, United States of America

Nanda D Sinha