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Our Trilaciclib API intermediate portfolio offers high-performance building blocks for the synthesis of the first-in-class, FDA-approved CDK4/6 inhibitor designed to protect bone marrow during chemotherapy. Trilaciclib (a kinase inhibitor used to reduce chemotherapy-induced myelosuppression) requires high-purity building blocks. Trilaciclib Advanced Intermediate 1 (CAS 2170746-95-7) & Trilaciclib Spiro-Core 2 (CAS 866620-36-2) represent critical milestones in the convergent synthesis of the spiro-pyrazino-pyrrolo-pyrimidine scaffold. Int -1 is synthesized through the condensation of 2-(methylthio)-7H-pyrrolo[2,3-d]pyrimidine-6-carboxylic acid and 1-aminomethyl-1-cyclohexanol. Int - 2 is then produced via a base-catalyzed internal cyclization of Intermediate 1, effectively locking the spiro-cyclohexane ring into the pyrazino-pyrrolo-pyrimidine framework. This "protection-free" methodology is preferred in 2026 for its high atom economy and reduced step-count compared to the original research routes. We utilise advanced spirocyclic construction and regioselective amination protocols to ensure these intermediates meet the stringent impurity profiles required for GMP-compliant drug substance manufacturing. Our manufacturing infrastructure is engineered for process safety and scalability, delivering high-purity solids with consistent (PSD). We are established global Trilaciclib intermediates supplier at 99%+ purity, ensuring minimal carry-over of methylthio-related impurities in the final API, and a broad range of various pharmaceutical intermediates for API manufacturers and semi-finished formulation suppliers, providing comprehensive analytical (HPLC/NMR/MS) and supporting quality assurance documentation (COA/TDS/SDS) across all grades, detailed impurity mapping; and region-specific regulatory support. We ensure reliable lead times from R&D quantities through commercial-scale manufacturing, enabling partners to meet diverse global and regional requirements.
Our Trilaciclib API intermediate portfolio offers high-performance building blocks for the synthesis of the first-in-class, FDA-approved CDK4/6 inhibitor designed to protect bone marrow during chemotherapy. Trilaciclib (a kinase inhibitor used to reduce chemotherapy-induced myelosuppression) requires high-purity building blocks. Trilaciclib Advanced Intermediate 1 (CAS 2170746-95-7) & Trilaciclib Spiro-Core 2 (CAS 866620-36-2) represent critical milestones in the convergent synthesis of the spiro-pyrazino-pyrrolo-pyrimidine scaffold. Int -1 is synthesized through the condensation of 2-(methylthio)-7H-pyrrolo[2,3-d]pyrimidine-6-carboxylic acid and 1-aminomethyl-1-cyclohexanol. Int - 2 is then...
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Pharmaceutical
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Pharmaceutical Actives & Precursors
Intermediates & Precursors
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Chemical Properties & Specifications
Skin Irrit. 2 (100%), Eye Irrit. 2 (100%), STOT SE 3 (100%)
P261, P264, P264+P265, P271, P280, P302+P352, P304+P340, P305+P351+P338, P319, P321, P332+P317, P337+P317, P362+P364, P403+P233, P405, and P501
CDK4/6 Inhibitor Synthesis: These intermediates are fundamental to constructing the complex spiro-structure of Trilaciclib, ensuring the correct spatial orientation for kinase binding. Oncology Drug Discovery: Essential for medicinal chemists developing next-generation myeloprotection agents and small-molecule inhibitors. Trilaciclib 1 & 2 intermediates are fundamental to constructing the complex spiro-structure of Trilaciclib, ensuring the correct spatial orientation for kinase binding Supply Chain De-risking: Our backward-integrated manufacturing ensures a steady supply of Int-1, reducing the complexity of multi-step API synthesis for pharmaceutical manufacturers.
Essential for medicinal chemists developing next-generation myeloprotection agents and small-molecule inhibitors
Int-2 serves as the reactive chlorinated scaffold ready for palladium-catalysed cross-coupling or nucleophilic aromatic substitution (SNAr)
Our backward-integrated manufacturing ensures a steady supply of Int-1, reducing the complexity of multi-step API synthesis for pharmaceutical manufacturers
Chemical Name: 2-Chloro-7,8-dihydro-6H-spiro[cyclohexane-1,9'-pyrazino[1',2':1,5]pyrrolo[2,3-d]pyrimidin]-6-one
The construction of the spiro-cyclohexane-pyrazino-pyrrolo-pyrimidine system is sensitive to reaction conditions. We utilize optimized cyclization parameters to ensure quantitative formation of the spiro-ring while maintaining the integrity of the pyrimidinone core. Our in-process controls (IPC) utilize high-resolution HPLC and LC-MS to monitor for ring-opening byproducts or unreacted precursors, ensuring a high-purity "clean" scaffold for your next step.
For Intermediate-1, we implement a stringent purification protocol to eliminate residual 1-methylpiperazine and pyridyl amine precursors. Given that Int-1 is a late-stage intermediate, we provide Impurity Mapping for any related substances above 0.1%. This transparency allows your regulatory teams to streamline the DMF (Drug Master File) filing process.
Our infrastructure is designed for telescoped reactions where possible to increase yield and reduce waste. We have specialised expertise in handling the heterocyclic amination required to convert Intermediate-2 to Intermediate-1. By optimizing the catalyst load and solvent recovery, we offer a commercially efficient alternative to traditional laboratory-scale synthesis, with lead times of 6–8 weeks for multi-kilogram batches.
Both Intermediate-1 and Int-2 are evaluated under ICH accelerated stability conditions. We ship in high-density polyethylene (HDPE) containers with double anti-static liners, vacuum-sealed under nitrogen where required. Every shipment includes a re-test date based on real-time stability data to ensure your R&D or manufacturing timelines are never compromised by degradation.
