The introduction of the very hydrophilic hydroxyl group can cause some metabolism-related troubles which can be circumvented by constrained structures and hindered groups.
To help medicinal chemists save time in their research programs, SpiroChem has designed SpiroKit 6 compiling 54 constrained amino alcohol derivatives.
Subsets 6c, 6d and 6e focuses on amino alcohols with OH shielding to prevent conjugation reactions:
Fused, bridged and spiro derivatives give access to 3D structures with improved properties:
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