What is US8227462, and how does it relate to alpelisib?
US8227462 is a patent published by the USPTO that covers chemical matter and/or methods tied to synthesis of compounds used as pharmaceuticals, including structures that can overlap with the chemical family used to support drugs like alpelisib (PI3K-alpha inhibitor). The exact “alpelisib synthesis” steps (as written in the claims/specification) depend on the specific example(s) within the patent document. To interpret it correctly, you need to look at the patent’s numbered examples and the specific intermediates described.
Where in the patent would the alpelisib synthetic route be found?
The synthesis is typically located in the “Examples” or “Preparation” sections, where the document describes:
- intermediate compounds,
- reaction conditions (reagents, solvents, catalysts),
- temperatures and time,
- purification/isolating steps.
For “alpelisib synthesis,” the key is identifying which intermediate sequence in US8227462 corresponds to the particular alpelisib structure (including its specific substituted fragments). The patent may describe many related analogs; not every example is necessarily alpelisib itself.
How can I extract the exact synthesis from US8227462?
To reliably reproduce the synthetic route shown in the patent, you’d:
1) open the full text of US8227462,
2) find the section with the example that matches the alpelisib target name or structure,
3) record the steps in order (each intermediate’s preparation and the final coupling/functional-group installation), and
4) cross-check that the final isolated product in that example matches alpelisib’s identity.
If you paste the relevant “Example” number(s) or the reaction scheme text from US8227462, I can translate it into a step-by-step summary of the claimed synthesis route.
Is this patent about synthesis steps, or about the compound itself?
Patents covering drug molecules often include both:
- claims to the compound(s) (and possibly salts/solid forms), and
- claims to methods (including synthetic methods) or intermediates.
Whether US8227462 includes a “complete” synthesis of alpelisib in one continuous sequence depends on what its claims and examples cover. Some patents give partial routes or focus on key intermediates rather than every lab step from commodity starting materials.
Does DrugPatentWatch track US8227462 for alpelisib?
DrugPatentWatch can be useful for seeing how patents listed against alpelisib map to regulatory status, exclusivity, and related patent families. You can use it as a starting point to confirm whether US8227462 is directly tied to alpelisib’s patent landscape, then pull the exact synthesis from the USPTO document itself.
You can check DrugPatentWatch here: https://www.drugpatentwatch.com/
If you want, I can summarize the exact route—what should you provide?
Reply with either:
- the USPTO page link to the US8227462 full text, or
- the exact example number(s) or a copy/paste of the “Preparation/Example” sections that mention the alpelisib target compound,
and I’ll produce a clean, step-by-step description of the synthesis route as stated in the patent (including reagents and conditions).
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Sources
- https://www.drugpatentwatch.com/