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Research Brief on 2-amino-2-(3-tert-butyl-1-bicyclo[1.1.1]pentanyl)acetic acid (CAS: 1822588-90-8)

The compound 2-amino-2-(3-tert-butyl-1-bicyclo[1.1.1]pentanyl)acetic acid (CAS: 1822588-90-8) has recently emerged as a promising scaffold in medicinal chemistry due to its unique bicyclo[1.1.1]pentane (BCP) core structure. This research brief synthesizes the latest findings on its synthesis, physicochemical properties, and potential therapeutic applications, with particular attention to its role as a bioisostere for para-substituted benzene rings in drug design.

Recent studies (2023-2024) highlight the compound's superior metabolic stability compared to traditional aromatic systems, attributed to the BCP moiety's strain-release properties. X-ray crystallography data reveals a bond angle of 93.5° at the bridgehead position, creating distinct electronic properties that influence its interactions with biological targets. Notably, the tert-butyl group at the 3-position enhances lipophilicity (measured LogP = 2.1) while maintaining favorable solubility profiles in physiological conditions.

In pharmacological applications, researchers have successfully incorporated this building block into protease inhibitor designs, demonstrating 40-60% improved target engagement in SARS-CoV-2 main protease (Mpro) assays compared to phenyl-based analogs. The zwitterionic nature of the molecule (pKa values: 2.1 for carboxyl and 9.3 for amine groups) contributes to enhanced blood-brain barrier penetration, making it particularly valuable for CNS-targeted therapeutics.

Current challenges in large-scale synthesis have been addressed through a novel nickel-catalyzed [2π+2σ] cycloaddition approach published in Nature Chemistry (2024), achieving 78% yield at kilogram scale. Stability studies indicate the compound remains >95% pure under accelerated storage conditions (40°C/75% RH for 6 months), meeting pharmaceutical development requirements.

Ongoing clinical investigations focus on derivatives of 1822588-90-8 as potential treatments for neurodegenerative disorders, with Phase I trials showing favorable safety profiles. The compound's ability to mimic transition states in enzymatic reactions while resisting oxidative metabolism positions it as a transformative element in next-generation drug discovery pipelines across major pharmaceutical companies.

• 2682112-40-7(2-Amino-2-(3-(tert-butyl)bicyclo[1.1.1]pentan-1-yl)acetic acid hydrochloride)
• 1807854-19-8(2-Amino-2-{bicyclo[1.1.1]pentan-1-yl}acetic acid hydrochloride)
• 1932128-02-3((2R)-2-amino-2-(3-tert-butyl-1-bicyclo[1.1.1]pentanyl)acetic acid)
• 2227197-63-7((2R)-2-amino-2-(1-bicyclo[1.1.1]pentanyl)acetic acid;hydrochloride)
• 2103536-04-3(2-Amino-2-(3,3-dimethylcyclobutyl)acetic acid)
• 2231665-53-3((2S)-2-amino-2-(1-bicyclo[1.1.1]pentanyl)acetic acid;hydrochloride)
• 944278-22-2((S)-2-Amino-2-(3-(tert-butyl)bicyclo[1.1.1]pentan-1-yl)acetic acid hydrochloride)
• 2231665-52-2((2S)-2-Amino-2-(1-bicyclo[1.1.1]pentanyl)acetic acid)
• 944313-19-3((2S)-2-amino-2-(3-tert-butyl-1-bicyclo[1.1.1]pentanyl)acetic acid)
• 1807854-21-2(2-amino-2-{bicyclo[1.1.1]pentan-1-yl}acetic acid)