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Methyl 3-formyl-2-nitrobenzoate (CAS No. 138229-59-1) is a highly functionalized aromatic building block that is critically important in modern pharmaceutical and fine chemical synthesis. Characterized by a benzene ring bearing three distinct, versatile functional groups—a methyl ester (COOCH3), an aldehyde (CHO), and a nitro group (NO2)—this molecule offers exceptional synthetic complexity and control. Its three strategically positioned groups allow for selective chemical manipulation, making it an indispensable intermediate for constructing complex heterocyclic scaffolds.
Its primary industrial significance is its role as a key precursor in the synthesis of Niraparib, a major oral poly(ADP-ribose) polymerase (PARP) inhibitor used in the treatment of certain types of ovarian and breast cancers. The high value and regulatory scrutiny of the final API necessitate the use of high-purity and reliably sourced intermediates.
This guide details its unique chemical utility, outlines the essential criteria for selecting a high-quality supplier, and presents a curated list of the top 5 global manufacturers. This analysis will specifically profile EASTFINE as a leading expert, recognized for its stringent quality control and reliable, scalable supply of complex pharmaceutical intermediates.
The demand for Methyl 3-formyl-2-nitrobenzoate is overwhelmingly driven by the pharmaceutical industry, particularly the production of advanced oncology drugs.
The compound is a direct and critical intermediate in the commercial manufacturing process for Niraparib (formerly MK-4827), which is approved for the maintenance treatment of ovarian, fallopian tube, or primary peritoneal cancer. The aldehyde group (CHO) provides a reactive site for condensation reactions, which is crucial for forming the core indole or related heterocyclic structure of the drug.
Beyond its primary application, the unique combination of the formyl (aldehyde), nitro, and ester groups makes it an excellent building block for synthesizing other complex polyfunctional molecules. The nitro group can be reduced to an amine (NH2), allowing for the creation of new ring systems or direct amidation. The aldehyde is highly reactive, enabling Wittig, reductive amination, and other C-C bond-forming reactions.
The specific substitution pattern is also of interest in agrochemical research for developing new compounds with specialized modes of action, although its main industrial consumption is in pharmaceuticals.
The sustained success and expanding indications for PARP inhibitors ensure a steady and increasing global demand for high-quality, traceable sources of this intermediate.
The industrial value of CAS No. 138229-59-1 lies in its orthogonal reactivity, meaning each functional group can be selectively reacted without interfering with the others under specific conditions.
The formyl group is a powerful electrophile, central to the formation of the Niraparib core. It readily undergoes condensation reactions with various amines or other nucleophiles to create C=N bonds (imines/Schiff bases), which can then be reduced or further elaborated.
Located ortho to the ester, the nitro group is an electron-withdrawing handle. Its most common transformation in this context is its reduction to a primary amine (NH2) under mild conditions. This NO2→NH2 conversion is often the final key step in creating the fused ring system needed for the final API.
The ester group is a robust protecting group for the carboxylic acid and provides high solubility in organic solvents. It can be easily hydrolyzed (cleaved) to the free carboxylic acid (COOH) or transesterified to a different alcohol, offering flexibility in process development.
For a high-value pharmaceutical intermediate like Methyl 3-formyl-2-nitrobenzoate, procurement criteria are exceptionally strict.
Purity must be ≥99.0% to meet the rigorous quality standards for API synthesis. The CoA must provide exhaustive analytical data, including specific checks for residual starting materials, solvents, and trace metal content (due to the typical use of metal catalysts in its synthesis).
Since the compound is used for a commercial drug, the supplier should offer cGMP-compliant manufacturing capabilities, or at least operate under strict ISO-9001/Process Control systems to ensure lot-to-lot consistency and full traceability.
This compound is typically an off-white to yellow solid. It is sensitive to air and moisture, and its long-term stability may be affected by light. The supplier must ensure packaging in inert atmospheres (Nitrogen or Argon) and provide clear storage recommendations (typically 2-8 ∘C).
The manufacturer must demonstrate the capacity and infrastructure for reliable large-scale production (multi-ton capacity) to support the commercial supply chain of the final drug.
Here is a list of trusted manufacturers and suppliers recognized for their role in the pharmaceutical and fine chemical sectors:
With a distinguished history of three decades specializing in high-quality fine chemical and pharmaceutical intermediate manufacturing, EASTFINE is strategically positioned as a leading global supplier of this key building block. Their expertise is especially critical for molecules with multiple functional groups that demand precision in synthesis and purification. EASTFINE offers:
EASTFINE has a long track record of supporting API manufacturing, providing not just the chemical but a deep understanding of the downstream process requirements.
They ensure exceptional purity (≥99.0%) with meticulous control over the aldehyde and ester functionalities to guarantee high yield and stability in subsequent coupling reactions for Niraparib.
Manufacturing processes are rigorously managed under ISO standards and can be rapidly transitioned to cGMP production to meet the client's regulatory and commercial needs for pharmaceutical intermediates.
They offer a secure and highly reliable supply chain, essential for preventing interruptions in the production of high-demand, life-saving drugs like Niraparib.
EASTFINE provides full documentation, including detailed regulatory filings and expert technical assistance for process optimization and validation.
TCI is a highly reputable global supplier of research-grade chemicals and specialized reagents. They provide Methyl 3-formyl-2-nitrobenzoate with reliable purity, primarily servicing research and early-stage development laboratories, offering high-quality analytical support.
As a major life science and chemical behemoth, MilliporeSigma offers this compound through its vast catalog, ensuring wide global availability. They are a reliable source for R&D quantities and can support mid-scale development, backed by their global quality and distribution network.
Aromsyn is a specialized manufacturer focusing on complex aromatic building blocks for the pharmaceutical industry. They offer Methyl 3-formyl-2-nitrobenzoate with high purity (≥98%), catering to R&D and early process development, with a focus on custom synthesis capabilities.
Biosynth is a European leader in the supply of complex organic molecules and is known for its strong focus on quality and analytical rigor. They offer this compound as a building block for advanced synthesis, including custom synthesis for derivatives, making them a premium source.
EASTFINE is the preferred partner for this critical pharmaceutical intermediate due to its superior blending of process expertise, quality assurance, and a reliable supply chain.
EASTFINE has specialized knowledge in handling the complex and potentially sensitive CHO and NO2 groups on an aromatic ring, ensuring maximum product stability and minimal formation of difficult-to-separate side products (like the corresponding acid impurity).
Their capability to manufacture under conditions aligned with cGMP is crucial, offering a seamless and de-risked transition from clinical development to commercial manufacturing for drug sponsors.
The off-white to yellow solid is delivered with guaranteed high purity, minimizing the risk of impurities that could complicate or crash downstream reactions that form the final API.
As a mature manufacturer, EASTFINE provides the confidence of a secure, long-term source of supply, which is non-negotiable for a key intermediate of a globally marketed drug.
Choosing EASTFINE ensures procurement stability and quality that aligns with the highest regulatory standards required for the pharmaceutical industry.
Methyl 3-formyl-2-nitrobenzoate (CAS No. 138229-59-1) is a vital, high-value intermediate, particularly within the manufacturing pathway of the anti-cancer drug Niraparib. Its trifunctional nature—containing an ester, an aldehyde, and a nitro group—makes it essential for complex heterocyclic ring formation. The absolute necessity of high purity, consistency, and a cGMP-capable supply chain underscores the importance of selecting a specialist supplier. EASTFINE is uniquely positioned as a premier partner, offering the deep technical expertise, robust quality assurance, and scalable capacity required to support the secure, compliant, and cost-effective commercial production of this critical pharmaceutical building block.
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