(2S)-1-tert-butoxycarbonyl-2-methyl-pyrrolidine-2-carboxylic acid

(2S)-1-(tert-Butoxycarbonyl)-2-methylpyrrolidine-2-carboxylic acid (also known as N-BOC-2-methyl-L-proline, Molecular Formula: C₁₀H₁₇NO₄; CAS No.: 103336-06-7) is a key chiral intermediate for pharmaceutical synthesis, and notably serves as a critical intermediate for Daridorexant (a novel dual orexin receptor antagonist clinically indicated for the treatment of adult insomnia). Its chemical structure is characterized by a methyl substituent at the 2-position of the pyrrolidine ring and a tert-butoxycarbonyl (BOC) protecting group on the pyrrolidine nitrogen atom. Under ambient temperature and pressure, it exists as a white to pale yellow solid, slightly soluble in water but soluble in polar organic solvents such as acetonitrile and methanol.

Strict quality control specifications are established for it: appearance compliance is verified by visual inspection; related substances (individual impurity ≤ 0.5%, total impurities ≤ 2.0%) and purity (≥ 98.0%) are determined by HPLC; enantiomeric excess (≥ 99.0%) is detected by chiral HPLC; moisture content is controlled to ≤ 1.0% via Karl Fischer titration (Method 1 of ChP 2020 Edition, Part IV). The recommended storage condition is sealed preservation at room temperature, with a retest period of 24 months. The aforementioned quality control and storage requirements ensure the batch-to-batch consistency and stability of the compound, providing reliable support for its industrial application in pharmaceutical synthesis including Daridorexant production.

The recommended storage condition is sealed preservation at room temperature, with a retest period of 24 months.