Non-polar and polar leaving groups
AssigneeBayer Pharma Aktiengesellschaft
InventorsKeith Graham, Mathias Berndt, Dae Yoon Chi, Byoung Se Lee, Sandip S. Shinde, Hee Seup Kil, Sang Ju Lee, Jin-Sook Ryu, Seung Jun Oh
Life of this patent
Estimating the term…
Abstract
The present invention provides novel and advantageous processes for preparing and purifying pharmaceuticals The processes comprise a nucleophilic reaction wherein a modified leaving group LM, which has increased lipophilicity, of a vector in a nucleophilic reaction which offers a convenient and time-saving way to purify the product from non-reacted precursors vector-LM and by-products LM.
Claims11
A method of preparation of compound of Formula II by direct nucleophilic radiofluorination of compound of Formula I
- wherein
- the difference between the logD of compound of Formula I and the logD of compound of Formula II is greater than 1.5,
- the vector is a targeting vector, and
- LM is a modified leaving group, suitable for direct nucleophilic fluorination,
- X is a nucleophilic moiety, preferably 18F.
A compound of Formula I:
- vector-LM I
- that is a precursor for a direct nucleophilic radiofluorination compound of Formula II:
- vector-X II
- wherein
- the difference between the logD of compound of Formula I and the logD of compound of Formula II is greater than 1.5, and
- vector is a targeting vector,
- X is a nucleophilic moiety preferably 18F and
- LM is a modified leaving group suitable for direct nucleophilic fluorination.
A modified leaving group LM is selected from
Dependencies are inferred from the claim text.