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1. (WO2018041985) CHEMOSELECTIVE THIOL-CONJUGATION WITH ALKENE OR ALKYNE-PHOSPHONAMIDATES

Pub. No.:    WO/2018/041985    International Application No.:    PCT/EP2017/071937
Publication Date: Fri Mar 09 00:59:59 CET 2018 International Filing Date: Sat Sep 02 01:59:59 CEST 2017
IPC: A61K 47/68
A61K 47/64
A61K 47/54
C07K 14/82
C07K 1/107
C07K 1/113
C07K 1/13
C07K 1/22
Applicants: FORSCHUNGSVERBUND BERLIN E.V.
LUDWIG-MAXIMILIANS-UNIVERSITÄT MÜNCHEN
Inventors: CHRISTIAN, Hackenberger
KASPER, Marc André
GLANZ, Maria
SAUER, Tom
SCHUMACHER, Dominik
HELMA-SMETS, Jonas
LEONHARDT, Heinrich
STENGL, Andreas
Title: CHEMOSELECTIVE THIOL-CONJUGATION WITH ALKENE OR ALKYNE-PHOSPHONAMIDATES
Abstract:
Disclosed are novel conjugates and processes for the preparation thereof. A process for the preparation of alkene- or alkyne-phosphonamidates comprises the steps of (I) reacting a compound of formula (III), with an azide of formula (IV), to prepare a compound of formula (V), reacting a compound of formula (V) with a thiol-containing molecule of formula (VI), resulting in a compound of formula (VII).