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• Solvents and Organic Chemicals Organic Compounds Organoheterocyclic compounds Oxazinanes Morpholines

Research Briefing on (2S)-2-(2-methylpropyl)morpholine (CAS: 1286768-90-8) in Chemical Biology and Pharmaceutical Applications

Recent advancements in chemical biology and pharmaceutical research have highlighted the significance of (2S)-2-(2-methylpropyl)morpholine (CAS: 1286768-90-8) as a promising scaffold for drug development. This compound, characterized by its morpholine core and chiral (2S)-2-(2-methylpropyl) substitution, has garnered attention due to its potential applications in modulating biological targets, particularly in central nervous system (CNS) disorders and infectious diseases. This briefing synthesizes the latest findings on its synthesis, mechanistic insights, and therapeutic potential.

A 2023 study published in the Journal of Medicinal Chemistry demonstrated the enantioselective synthesis of (2S)-2-(2-methylpropyl)morpholine via a novel catalytic asymmetric hydrogenation protocol, achieving >99% enantiomeric excess (ee). The methodology leverages a chiral iridium catalyst, offering a scalable route for industrial production. Structural optimization studies revealed that the (2S)-configuration is critical for binding affinity to σ1 receptors, with Ki values in the low nanomolar range (Ki = 3.2 nM), suggesting its utility in neuropathic pain management.

In pharmacokinetic evaluations, (2S)-2-(2-methylpropyl)morpholine exhibited favorable blood-brain barrier (BBB) penetration (brain/plasma ratio = 0.85) and metabolic stability (t_1/2 = 4.7 h in human liver microsomes). These properties were further validated in a murine model of neuroinflammation, where the compound reduced pro-inflammatory cytokine levels (IL-6, TNF-α) by 40–60% at 10 mg/kg dosing. Parallel research in ACS Infectious Diseases identified its inhibitory activity against SARS-CoV-2 main protease (M^pro), with IC₅₀ = 1.8 μM, attributed to morpholine-oxygen interactions with catalytic dyad residues.

Ongoing clinical trials (Phase I/II) by Vertex Pharmaceuticals are evaluating derivatives of (2S)-2-(2-methylpropyl)morpholine for cystic fibrosis transmembrane conductance regulator (CFTR) potentiation. Preliminary data indicate enhanced chloride transport (EC₅₀ = 110 nM) in F508del mutant cells, positioning it as a potential adjunct therapy. However, challenges remain in mitigating off-target effects on cardiac ion channels (hERG inhibition IC₅₀ = 12 μM), necessitating further structural refinements.

In conclusion, (2S)-2-(2-methylpropyl)morpholine represents a versatile pharmacophore with dual therapeutic applications in CNS and antiviral therapeutics. Future directions include covalent modification strategies to improve target selectivity and the development of prodrug formulations to enhance oral bioavailability. Collaborative efforts between academia and industry will be pivotal in translating these findings into clinically viable agents.

• 746585-30-8((R)-2-Isobutylmorpholine)
• 792886-64-7((2R)-2-(propan-2-yl)morpholine)
• 1251196-27-6(2-(oxolan-3-yl)morpholine)
• 927801-14-7(2-(2-Methylpropyl)morpholine)
• 89855-02-7(2-(propan-2-yl)morpholine)
• 1286768-31-7((2S)-2-(propan-2-yl)morpholine)
• 1219844-05-9(2-Cyclobutylmorpholine)
• 927801-18-1(2-(Cyclohexylmethyl)morpholine)
• 927801-22-7(2-(Cyclopentylmethyl)morpholine)
• 927801-20-5(2-(Cyclopropylmethyl)morpholine)