IP Library › Granted Patent US 7,851,621
Granted Patent B2
US 7,851,621 · App. 11/993,185 · Granted Dec 14, 2010

Synthesis of deoxybiotinyl hexamethylenediamine-dota

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Quick Facts
Patent No.
US 7,851,621
App. No.
11/993,185
Granted
Dec 14, 2010
Kind
B2
Abstract

A process for the synthesis of deoxybiotinyl hexamethylenediamine0-DOTA is herein described. Said process comprises reacting biotinyl hexamithylenediamine with tri-t-butyl DOTA in the presence of benzotriazol-1-yl-oxytripyrrolidinophosphonium hexafluorophosphate, as the condensing agent, and triethylamine, as a base.

Claims (4)

1. Process for synthesising deoxybiotinyl hexamethylenediamine-DOTA comprising reacting biotinyl hexamethylenediamine with tri-t-butyl-DOTA in the presence of benzotriazol-1-yl-oxytripyrrolidinophosphonium hexafluorophosphate, as the condensing agent, and triethylamine, as the base.

2. Process according to claim 1 , in which biotinyl hexamethylenediamine is reacted with tri-t-butyl-DOTA in an organic solvent.

3. Process according to claim 2 in which the organic solvent is dichloromethane.

4. Process according to claim 1 , involving a subsequent step of hydrolysis in an aqueous environment with an acid pH.

Assignments (3)
CHANGE OF ADDRESS Recorded Oct 15, 2019
From: ALFASIGMA S.P.A.
To: ALFASIGMA S.P.A.
Reel/Frame 050727/0652 →
MERGER Recorded Nov 14, 2017
From: SIGMA-TAU INDUSTRIE FARMACEUTICHE RIUNITE S.P.A.
To: ALFASIGMA S.P.A.
Reel/Frame 044760/0906 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Feb 19, 2008
From: MARZI, MAURO; DI MARZO, MARIA
To: SIGMA-TAU INDUSTRIE FARMACEUTICHE RIUNITE S.P.A.
Reel/Frame 020527/0718 →