Boc-Pro-NH2

Boc-Pro-NH₂ is a protected L-proline derivative characterized by a tert-butyloxycarbonyl group on the pyrrolidine nitrogen and a primary amide at the C2 position. As a chiral building block, Boc-Pro-NH₂ provides the rigid pyrrolidine scaffold that is extensively employed in the synthesis of peptidomimetics and bioactive compounds. The Boc protecting group of Boc-Pro-NH₂ enables orthogonal deprotection under acidic conditions (e.g., TFA), while the primary amide serves as a versatile functional group for further derivatization. Boc-Pro-NH₂ is supplied as a white to off-white crystalline powder with a melting point of 104–108 °C and ≥97–98% purity. In pharmaceutical research, Boc-Pro-NH₂ serves as a key intermediate in the preparation of thiazole amide peptidomimetics and other biologically active compounds. Boc-Pro-NH₂ is an indispensable building block for medicinal chemists developing proline-containing drug candidates and peptide-based therapeutics.

Product Parameters

Application

N-tert-butylcarbonyl-L-prosylamide serves as an intermediate in chiral organic synthesis and pharmaceutical molecule synthesis, and is used as a raw material for the development of vitagliptin (for type 2 diabetes) and the anticancer drug Leuprolide Acetate. Vglitacibrutin is a selective, competitive, and reversible DPP-4 inhibitor that promotes insulin production by pancreatic β-cells while reducing glucagon levels, thereby lowering blood glucose levels; it is primarily indicated for the treatment of type 2 diabetes.

Synthetic Route

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Dissolve BOC-L-proline (1.00 g, 4.65 mmol), diisobutyl dicarbonate (1.52 g, 6.97 mmol), ammonium bicarbonate (0.55 g, 6.97 mmol), and pyridine (1.0 mL) in dioxane (20 mL) and stir at room temperature for 6 hours. Upon completion of the reaction, extract the product with dichloromethane, wash the organic phase successively with 1 M hydrochloric acid and saturated sodium chloride solution, dry it with anhydrous sodium sulfate, filter, and concentrate under reduced pressure. Add n-hexane (100 mL) to the concentrate and sonicate to precipitate the product as a white solid, yielding N-tert-butoxycarbonyl-L-prolamide (0.85 g, yield 85%). The product was characterized by 1H NMR (300 MHz, CDCl₃): δ 4.37–4.34 (m, ¹H); 3.47–3.36 (m, ²H); 2.07–1.85 (m, ⁴H); 1.49 (s, ⁹H). Mass spectrometry (ESI) showed m/z 215 [M + H]⁺.

Product Quality Assurance

Cosperpharm has established a comprehensive quality assurance system for Boc-Pro-NH₂ that meets the rigorous expectations of medicinal chemistry and pharmaceutical research applications:

Thorough analytical characterization. Each batch undergoes multi-technique analytical release testing: HPLC purity (≥97–99% with full chromatographic traceability), melting point confirmation (104–108 °C), appearance verification (white to off-white powder), and identity confirmation by NMR and mass spectrometry where applicable.

Full batch traceability with retention samples. From raw material procurement through Boc protection, purification, crystallization, drying, and final packaging, every step is fully documented and traceable. Each batch receives a unique lot number with sufficient retention samples maintained in accordance with Cosperpharm quality procedures.

Stability monitoring program. Cosperpharm conducts ongoing stability studies under recommended storage conditions. Shelf life: 3 years at –20 °C; 2 years at 4 °C.

Documentation ready for research use. Every shipment includes a Certificate of Analysis (COA) with batch-specific purity and characterization data, and customs documentation for international delivery. Custom quality documentation is available upon request.

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