CGP-7930

CGP-7930 was the first positive allosteric modulator of GABA_B receptors described in literature. CGP7930 is also a GABA_A receptor positive allosteric modulator and a blocker of Potassium channels.
CGP7930 was developed in Novartis and has been used extensively for scientific research. It has anxiolytic effects in animal studies, and has a synergistic effect with GABA_B agonists such as baclofen and GHB, as well as reducing self-administration of alcoholic drinks and cocaine.
CNS Review:

Synthesis

The chemical synthesis has been described: Starting material: Product of first step:
2,6-Di-tert-butylphenol is treated with formaldehyde, base and methanol to give . Base catalyzed reaction with isobutaldehyde gives CGP-13501. Hydride reduction of the aldehyde gives the primary alcohol.
According to Krysin, 2,6-Di-tert-butylphenol is reacted with Neopentyl glycol with lye in an autoclave. Although 1 step reaction, yield was quoted as merely 15%.