L-tert-Leucine;

CAS No.: 20859-02-3

Molecular Formula: C₆H₁₃NO₂ Molecular Weight: 131.17 EINECS No.: 424-750-7

Applications of L‑tert‑Leucine:

• Anti-HIV drugs (Atazanavir)

  An essential side chain for synthesizing protease inhibitors, which significantly improves the drug’s resistance to enzymatic hydrolysis and bioavailability.

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• Anti-hepatitis C drugs (Boceprevir, Telaprevir)

  Incorporation into the molecule enhances binding affinity to viral proteases and prolongs the in vivo half-life.

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• Anticancer / antitumor drugs

  Used in the synthesis of targeted drugs such as GCP-75136 and various peptide-based anticancer pharmaceuticals.

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• Others

  An important intermediate for synthesizing new drugs for antidiabetic, antibacterial, and antifungal applications.

II. Synthesis of Peptide and Protein Drugs

• Stabilizing peptide conformation

  The strong steric hindrance of the tert-butyl group fixes the peptide chain conformation and greatly enhances the stability of α-helices / β-sheets.

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• Resistance to enzymatic degradation

  Peptides containing L-tert-leucine are difficult to degrade by proteases in vivo, with half-life increased several times.

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• Enhanced binding affinity

  Improves specific binding to receptors / enzymes, boosting efficacy and targeting.

III. Chiral Synthesis and Catalysis (High-End Applications)

• Chiral ligands (PHOX ligands)

  Used to synthesize highly efficient ligands such as (S)-tert-butyl PHOX for asymmetric catalytic hydrogenation, epoxidation, and other reactions.

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• Chiral catalysts / auxiliaries

  Prepares chiral copper polymers, thiazolidinethiones, etc., for catalytic kinetic resolution and free radical cyclization, with ee values > 99%.

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• Organic synthesis building blocks

  A key chiral unit for constructing complex chiral molecules and total synthesis of natural products.

IV. Other Applications

• Nutrition / feed: Used in small amounts as a nutritional fortifier and feed additive (non-primary use).
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• Reference standards: Chiral reference substances and impurity standards for pharmaceutical R&D.