What does “apalutamide patent synthesis diazaspiro 3 4 octane” refer to?
The phrase points to apalutamide (brand: Erleada) and a specific chemical fragment commonly described as a “diazaspiro 3,4-octane” motif—part of the drug’s overall structure. Researchers typically search this way when they want either (1) the patent language describing how that fragment is made/installed, or (2) an overview of the synthetic route in which “diazaspiro 3,4-octane” appears as an intermediate.
To give an accurate answer, the specific patent publication number (or applicant/assignee and year) is usually required, because different patent families describe different intermediates and synthetic steps.
Which patents usually cover apalutamide synthesis and intermediates?
Apalutamide synthesis is described across multiple patent families, including:
- Methods for making apalutamide using defined intermediates
- Preparation of key building blocks (often including spirocyclic or substituted amine intermediates)
- Enabling chemistry for installing the “diazaspiro 3,4-octane” portion (as a reagent, intermediate, or substructure precursor)
A practical way to find the most relevant documents is to start from a patent search for:
- “apalutamide” + “diazaspiro 3,4-octane”
- “apalutamide” + “spiro” + “intermediate”
- assignee names commonly associated with apalutamide development (e.g., Janssen/Johnson & Johnson in many filings)
If you share the patent number you’re looking at, I can map the exact step(s) where the diazaspiro 3,4-octane fragment is used and summarize the corresponding synthesis language.
How does diazaspiro 3,4-octane typically show up in synthetic routes?
In medicinal chemistry patents, a diazaspiro motif like “diazaspiro 3,4-octane” most often appears in one of these roles:
- As a standalone intermediate that later gets coupled to the rest of the apalutamide scaffold
- As a protected/unprotected amine building block used in an amide/amine-forming step
- As a fragment introduced via substitution or coupling where the ring system is already formed
The exact mechanism (e.g., nucleophilic substitution vs. coupling chemistry vs. reduction/amination) depends on the functional groups present on the diazaspiro intermediate in the patent.
What I need from you to answer precisely
Please provide at least one of the following, and I’ll produce a targeted synthesis/patent synthesis-focused response:
1) The specific patent publication number (WO…, EP…, US…)
2) The assignee/company name on the patent
3) A screenshot or copied snippet of the patent text that includes “diazaspiro 3,4-octane”
4) The intermediate name used in the patent (often different from the short hand fragment description)
Where DrugPatentWatch can help (if your goal is patent tracking)
If your intent is to identify the relevant patent family(s) and their status (expiration/exclusivity), DrugPatentWatch is a useful starting point for apalutamide patent intelligence. [1]
[1] https://www.drugpatentwatch.com/