Risdiplam intermediate

Lisi Puran Key Intermediate (Boc Protection Type) Product Information

nature

this intermediate is a Boc-protected late-stage advanced intermediate in the synthesis route of lisepran (Risdiplam). The molecule contains 4,7-diazaspiro [2.5] octane skeleton, imidazopyridazine fragment and pyridopyrimidinone fragment, with complex structure, dense nitrogen atoms and large aromatic heterocyclic conjugate system. The appearance is usually a white to bright yellow powder with a density of about 1.39g/cm³ (predicted), very low water solubility, very low vapor pressure, and exists and operates as a solid under normal conditions. The most critical chemical property is the acid sensitivity of Boc group: Boc deprotection can occur under acidic conditions, releasing tert-butyl cation and carbon dioxide, which is the chemical basis for it to be used as an intermediate in the final stage of lisipran synthesis, and also determines that its storage and process operation must be strictly protected from acid, moisture and light, and sealed and stored at 2-8°C.

Use

the product is a key late-stage intermediate in the synthesis of lisiprimonil API. Lisipramine is the world’s first RNA-targeted small molecule drug for the treatment of spinal muscular atrophy (SMA), which works by modifying SMN2 pre-mRNA splicing and increasing functional SMN protein levels. In the synthetic route, the Boc-protected intermediate is purified to obtain the Lisipran API after removing the Boc group under acidic conditions; therefore, it is the core process node connecting the advanced intermediate with the final API, and its purity, impurity spectrum and batch stability directly affect the quality and yield of the downstream API. In addition, it can also be used for the study of related impurities, process development and analytical methods.

Safety Information

the product belongs to R & D/industrial pharmaceutical intermediates, can not be used for human body. The public database includes it in the management of hazardous chemicals, and the purchase and transportation must meet the relevant qualifications and regulatory requirements of hazardous chemicals. Avoid inhalation of dust and direct contact with skin and eyes during operation. It is recommended to use appropriate personal protective equipment (protective gloves, goggles, lab coat) in a fume hood or closed operating environment. Storage must be strictly 2-8°C, sealed, protected from light, dry, and isolated from acids; acidic environment will trigger Boc deprotection and may lead to product degradation, so distribution, weighing and reaction feeding should avoid contact with acidic dishes, acidic solvents or humid air. The specific GHS classification, risk terminology and safe operating parameters shall be based on the SDS/COA/TDS provided by the supplier with the lot.

The advantages and capacity of our company in producing this product: why customers choose us

first, this is our regular commercial product, not a laboratory sample that can be done by accident. Shanghai Lizhuo (Lizhuo Pharmaceutical) has listed CAS 2133298-74-3 as a regularly production product, which can be stably supplied from small samples to batches above tonnage. For high-value, high-regulatory-threshold rare disease drug intermediates such as Lisi Puran, what customers really need is a continuous, repeatable, scalable source of supply, not a one-time gram sample.

Second, we have complete hardware and process depth from laboratory to industrial. The company has a 1,000 m² research and development laboratory, and the Wuhan pilot plant is equipped with 20 50 L-1000 L reactors and an ultra-low temperature reaction system up to − 120°C, with an amplification capacity from kilogram to ton. This means that the intermediate from route screening, impurity control to batch consistency verification can be completed in the same system, reducing the uncertainty and time cost in technology transfer.

Third, we have targeted process control capabilities for acid-sensitive Boc-protected late-stage intermediates. The core process difficulty of the product is that the Boc group is sensitive under acidic conditions, and the subsequent deprotection needs to be carried out accurately under acidic conditions. We have long focused on strict control of process parameters and batch stability in the field of high-purity pharmaceutical intermediates, with conventional purity specifications up to 98%(HPLC), and can provide customized quality standards and impurity research support based on customer needs.

Fourth, compliance documents and regulatory support are in place. We can provide COA, MSDS, TDS and other batch documents, and strictly follow the sales, packaging and transportation compliance requirements of hazardous chemicals. For products covered by patent status, the company explicitly sells only for research and development and compliance production purposes, helping customers reduce regulatory and intellectual property risks in the procurement process.

Fifth, product positioning is highly matched with customer needs. As an oral small molecule drug in the SMA field, the supply chain of LiSiPuLan has high requirements for the purity of intermediates, impurity control, supply continuity and cost controllability. We are not just a “supplier with goods”, but a high-tech enterprise with high value-added pharmaceutical intermediates research and development, process amplification and commercial production as the core competence, in anti-tumor, mental nerve, anti-virus, hypoglycemic and other fields have accumulated system experience from route development to ton delivery. The customer chooses us, in essence, to choose a manufacturing partner that can run through, scale up, and deliver late-stage key intermediates from the process.

At the production capacity level, in addition to Lisi Pulan intermediates, the company has recently achieved a number of high-value pharmaceutical intermediates industrial-scale production, and continue to demonstrate the reliable supply capacity of high-purity intermediates in international platforms such as CPHI. Specific to the current batch capacity, delivery cycle and customized packaging of CAS 2133298-74-3, welcome to contact us directly for confirmation.

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