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Piperidines, Piperazines & Morpholines

Piperidines, piperazines, morpholines and tetrahydroquinolines for CNS drugs, antihistamines, Mitsunobu chemistry and many amine-containing APIs in development.
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Saturated nitrogen rings are among the most common features of small-molecule drugs, adding basicity, solubility and three-dimensional shape. This sub-category supplies piperidines, piperazines, morpholines and partially saturated fused rings. Examples include (R)-Piperidin-3-ol and its hydrochloride, (S)-Ethyl nipecotate, 1,2,3,4-Tetrahydroisoquinoline, 1,2,3,4-Tetrahydroquinoline and 1,1′-(Azodicarbonyl)dipiperidine (ADDP), a Mitsunobu reagent.

For chiral piperidines such as 3-hydroxypiperidine and nipecotate esters, enantiomeric purity is the key figure because these units often carry the stereocentre into the API. Free bases are frequently liquids or low-melting solids that absorb carbon dioxide from air, so hydrochloride salts are offered for stability. Mono-protected piperazines let you functionalise one nitrogen at a time, which keeps routes short and avoids mixtures of mono- and di-substituted products.

Products ship sealed, under nitrogen where needed, from gram packs to kilograms. Each lot comes with a COA and SDS reporting purity and, for chiral items, optical data. Search by CAS to separate enantiomers and salt forms quickly.

Piperidines, Piperazines & Morpholines: questions buyers ask

What is ADDP and when is it used?
1,1′-(Azodicarbonyl)dipiperidine is an azo reagent used in Mitsunobu reactions in place of DEAD or DIAD. It works better with weakly acidic nucleophiles, such as some phenols and heterocycles, when paired with tributylphosphine. It is a solid, which makes it easier to handle than liquid azodicarboxylates.
Why buy (R)-piperidin-3-ol rather than the racemate?
Many drugs need a single enantiomer of the 3-hydroxypiperidine unit, for example in some kinase inhibitors. Starting with the correct enantiomer avoids resolution later and the loss of half the material. Check the ee on the COA, and choose the salt or free base form that suits your next step.
How do I functionalise just one nitrogen of a piperazine?
Use a mono-protected piperazine, such as a Boc or benzyl derivative, so only the free nitrogen reacts. After the first substitution, remove the protecting group to expose the second nitrogen. Alternatively, use a large excess of piperazine, but separation of mono- and di-substituted products is then needed.

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