3-Pyrrolidinecarboxylic acid, 4-(1,3-benzodioxol-5-yl)-2-(4-Methoxyphenyl)-, ethyl ester, (2α,3α,4α)-

3-Pyrrolidinecarboxylic acid, 4-(1,3-benzodioxol-5-yl)-2-(4-methoxyphenyl)-, ethyl ester, (2α,3α,4α)- is a high‑purity, chirally defined pharmaceutical intermediate supplied by Cosperpharm for the research, development, and manufacturing of selective endothelin receptor antagonists. As the core diarylpyrrolidine scaffold from which the clinically validated ETA antagonist Atrasentan (ABT-627) was derived, this 3-Pyrrolidinecarboxylic acid, 4-(1,3-benzodioxol-5-yl)-2-(4-methoxyphenyl)-, ethyl ester, (2α,3α,4α)- directly corresponds to the key building block that medicinal chemists at Abbott Laboratories transformed into a drug with IC₅₀ = 0.36 nM for ETA receptor binding and >1000-fold selectivity over ETB. Moreover, this 3-Pyrrolidinecarboxylic acid, 4-(1,3-benzodioxol-5-yl)-2-(4-methoxyphenyl)-, ethyl ester, (2α,3α,4α)- is employed as a critical process impurity and reference standard for analytical method development and quality control of Atrasentan and its analogs. At Cosperpharm, each batch of 3-Pyrrolidinecarboxylic acid, 4-(1,3-benzodioxol-5-yl)-2-(4-methoxyphenyl)-, ethyl ester, (2α,3α,4α)- is synthesized under rigorous stereochemical control and supplied with comprehensive analytical documentation to support both R&D and regulatory submissions.

Product Parameters

Why Cosperpharm?

Cosperpharm is a trusted partner for sourcing chirally defined pharmaceutical intermediates, offering a blend of technical expertise and supply chain reliability. Our facilities operate under GMP-aligned quality standards, with in‑house analytical capabilities including chiral HPLC, LC‑MS, NMR, and GC‑MS to ensure that every batch of 3-Pyrrolidinecarboxylic acid, 4-(1,3-benzodioxol-5-yl)-2-(4-methoxyphenyl)-, ethyl ester, (2α,3α,4α)- meets your exact stereochemical and purity specifications. We pride ourselves on transparency—each shipment includes a comprehensive Certificate of Analysis (COA) with HPLC purity data, mass spectrometry confirmation, and impurity profiling. Our technical support team provides responsive assistance for custom packaging, scale‑up inquiries, and regulatory documentation (including stability data for ANDA/DMF submissions). With competitive pricing, flexible packaging options, and a proven track record of on‑time deliveries to pharmaceutical partners worldwide, Cosperpharm is your reliable source for Atrasentan intermediates and reference standards.

Product Advantages

1.Precisely defined (2α,3α,4α) trans,trans stereochemistry – The three contiguous chiral centers are strictly controlled and verified by chiral HPLC. This stereochemistry is the validated pharmacophore that enabled Atrasentan to achieve an IC₅₀ of 0.36 nM at the ETA receptor with >1000‑fold selectivity over ETB.

2.Structurally validated diarylpyrrolidine core – The 2‑(4‑methoxyphenyl) and 4‑(1,3‑benzodioxol-5-yl) substitution pattern has been extensively optimized through structure‑activity relationship (SAR) studies at Abbott Laboratories, representing the optimal scaffold for potent ETA antagonism.

3.Ethyl ester for versatile late‑stage functionalization – The carboxylate ester provides a handle for amidation, reduction to the primary alcohol, or hydrolysis to the free acid, enabling the synthesis of diverse Atrasentan analogs and N‑substituted derivatives.

4.Multi‑faceted utility – Functions as a key synthetic intermediate for Atrasentan API manufacturing, a process impurity reference standard for quality control, and a research tool for ETA receptor antagonist drug discovery.

5.High purity with tightly controlled impurities – Each batch is tested to ≥98% purity by HPLC, with individual impurities ≤0.5% and total impurities ≤1.0%, ensuring consistent performance in both synthetic transformations and analytical method development.

6.Stable, handleable crystalline solid – Isolated as a white to off‑white solid, the compound is easy to weigh, store, and scale, with a documented shelf life of 24 months under recommended conditions.

7. Regulatory‑ready documentation – Each batch is supplied with complete characterization data (HPLC, MS, optional NMR) and stability studies to support Drug Master File (DMF) and Abbreviated New Drug Application (ANDA) submissions.

Frequently Asked Questions (FAQ)

Q1: What is the primary use of this compound?

A: It is a key chiral intermediate for the synthesis of Atrasentan (ABT-627), a highly selective ETA receptor antagonist developed for the treatment of diabetic nephropathy, chronic kidney disease, and certain cancers. It is also used as an impurity reference standard for analytical method development and quality control of Atrasentan API.

Q2: What is the endothelin receptor system?

A: Endothelin (ET) is a potent vasoconstrictor peptide with two major receptor subtypes, ETA and ETB. ETA receptors mediate vasoconstriction and cell proliferation, while ETB receptors are involved in vasodilation and clearance of ET-1. Selective ETA antagonists like Atrasentan are being developed for cardiovascular and renal indications.

Contact Us

Ready to advance your ETA antagonist program with 3-Pyrrolidinecarboxylic acid, 4-(1,3-benzodioxol-5-yl)-2-(4-methoxyphenyl)-, ethyl ester, (2α,3α,4α)-? Contact Cosperpharm today for a competitive quotation, product documentation, sample request, or a technical consultation with our experienced team.