The amino group is one of the most common features of active substances and are found in most drug candidates and marketed drugs. Amines are very useful handles for the coupling to other fragments and allow a very versatile range of transformations, such as amide bond formation, sulfonamide, N-arylations and alkylation. They are generally basic and this parameter is of importance for drug design, in particular in the field of CNS drugs. It is important for medicinal chemists to have access to the widest range of substituents on amines to modulate their pKa.
SpiroChem has developed a wide range of aliphatic amines, spirocyclic amines, conformationally restricted amines with substitutions such as externe groups, perfluoroalkyl chains and more, which allows for fine tuning of properties. Oxetanyl amines for example are almost neutral due to the presence of the externe group. We also have bulky amines, similar to adamantyl amine, with a variety of shapes and sizes, have a look at our range of bicyclo[x.y.z]alkanes. The bicyclo[1.1.1]pentyl-1-amine in particular is a very interesting surrogate for tert-butyl amine for example. It also allows for fine tuning of the logP and log D of your molecules.
Contact us for more details. We can design new series for you or help you introduce our fragments on your scaffold of interest.
We also offer those amines as kits, where a bespoke selection of commonly found amines are derivatized to allow for a quick screening of properties.
Working with SpiroChem allows you to save time on early synthetic work so that you can focus on high-value added transformations.
SpiroChem designs the tools, but YOU develop the drugs of tomorrow!