This issue of Enamine Product Focus highlights Lactams,
cyclic amide building blocks. There are numerous examples of Lactams
usage in drug discovery, e.g., β-lactam based antibiotics, oral
anticoagulant Rivaroxaban, and anticonvulsant Levetiracetam.
 |  |
| Rivaroxaban, 2008 | Levetiracetam, 2000 |
The specific features of
Lactam building blocks that are of advantage to drug design are summarized in the chart below.
Enamine’s Lactam
building block collection is represented by many useful scaffolds, for
example, piperidones, piperazinones, (thio)morpholiones, pyrrolidones,
and their benzo-fused analogues. From combinatorial chemistry standpoint
especially interesting lactams in our collection are those bearing
additional functionalities, such as carboxyl, chlorosulfonyl, and
amino-groups.
 |  |  |
| Piperidones | Piperazinones | Morpholinones |
 |  |  |
| Thiomorpholinones | Pyrrolidones | Dihydroquinoxalinones |
The procedures developed for the synthesis of our Lactams
allow preparation of highly diverse building blocks on 1–10 g scale. In
addition we offer synthesis of novel compounds of the requested
structure in 4–8 weeks. Scale-up to 1 kg quantity is performed upon
request.
Representative examples of our Lactam building blocks are given below.
Amines
Sulfochlorides
Carboxylic acids
Other Lactams
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