'Easy-to-synthesise molecules': how patentability screening filtered out false leaders before the lab

What we did

We built a screen of 22 candidate molecules along four axes — ease of synthesis, durability of demand, availability of domestic feedstock, and the patent angle — and ran the output through a separate loop of independent critical review. The conclusion proved both sobering and useful: for molecules with a simple synthesis the patent moat is weak by definition, and two of the top candidates had to be dropped or downgraded because of regulatory red flags invisible from a 'what's cheapest to make' viewpoint. We separated two tasks the client had reflexively treated as one, and screened out the false leaders before any spend on lab development.

The starting point

The client was preparing an entry into import substitution and reasoned along intuitive lines: the market is undersupplied — so take something simple and cheap to make from local feedstock and lock it down with a patent. The framing sounded like a single task — 'easy to synthesise and patent it'. In reality it fused two different ones: a market opportunity (the product isn't made in the country) and patentability (worldwide novelty). A product's absence from the market confers no right to a patent: a known molecule in the public domain cannot be patented — you can only protect what is added to it: a synthesis route, a polymorph or salt, a dosage form, a combination, a delivery device.

• The market backdrop heightened the temptation of 'simple' molecules: across the region up to 80% of pharmaceutical substances are imported, while domestic production covers only about 52% of the domestic market by value.
• Almost all of this domestic production (on the order of 94%) is generics, not originator drugs; total drug imports exceed $1 billion a year.
• The shortage is real — but that's exactly why it was important not to confuse a 'gap in the market' with a 'defensible business'.

What the analysis showed

Each molecule was scored on a combined 'quick-win' score: ease of synthesis × durability of demand × availability of local feedstock, with a separate column for the patent angle; the synthesis is simple and well-established for all of them — typically 1–3 steps, no exotic reagents and no complex sterile manufacturing. The top candidates scored roughly 4.3–4.7 out of 5 — high on 'ease and demand', but it was the analysis of the patent column that flipped the picture. That analysis produced two counter-intuitive findings and several corrections:

• The patent moat is weak by definition. The simpler and better-known the molecule, the less of it can be protected: for the top 'easy' entries a patent is possible only on the synthesis route or the dosage form — weak, easily circumvented protection. The real advantage lies not in intellectual property but in cheap local feedstock (large-tonnage local chemicals, forest-chemical and agricultural feedstock) that importers don't have. The entry strategy changes: not a 'patent monopoly' but a 'feedstock-cost advantage'.
• Regulatory landmine No. 1: a dual-use precursor. One of the nominal leaders on the 'ease + own feedstock' pairing turned out to be a dual-use precursor (its circulation is restricted in a number of jurisdictions) — as an investment target it is downgraded, not recommended.
• Regulatory landmine No. 2: a controlled precursor. For another group of simple candidates the key synthesis reagent is a controlled precursor whose procurement requires licensing and monitoring; this was entered as an explicit regulatory caveat rather than left as a hidden risk.
• Three corrected labelling errors. One 'synthesis' was in fact an isolation/extraction, not a synthesis; for two entries the availability of local feedstock had been overestimated and was downgraded to 'requires verification' status.
• The conclusions are robust. After all the corrections the top six synthesis leaders were unchanged, and no gross errors were found in the synthesis routes. The review did not destroy the result but cleaned it up: it stripped out false precision and surfaced the red flags.

The result

The client got not a list of 'what's fashionable to make' but a ranked list with an honest read on each candidate: where the advantage is in feedstock, where in a patent, and where a regulatory red flag stands. The practical payoff:

• Two 'false leaders' were screened out before any spend on lab development and feedstock procurement — not after the precursor requiring a licence would have surfaced at the supply stage.
• The very framing of the task was reformulated: 'easy to synthesise' ≠ 'a good business'. Market opportunity and patentability were pulled apart, and each was given its own logic of protection: a feedstock advantage for simple molecules, a patent on composition or device for finished forms.
• A sequence of actions was laid out, split by risk: a pilot on domestic feedstock (low risk, a cost advantage), a patentable finished form (medium risk, a standalone composition patent), a strategic direction with technology transfer (high risk, high ceiling).

Caveats and data status

What is verifiable, what is an estimate, and what needs confirmation — flagged explicitly.

• What is measured and verifiable: the synthesis routes, the number of steps and the nature of the reagents — from the chemical and patent literature; the regulatory status of the precursors — from public lists of controlled substances. These items are verifiable against primary sources.
• What is an estimate: market volumes in monetary terms — order-of-magnitude expert ranges based on the aggregated structure of imports, not customs-statistics data by commodity code. The scoring is a relative prioritisation with preset weights, not a financial model.
• What comes from the client and needs confirmation: the availability of domestic feedstock for a number of entries needs confirmation by actual contracts (for several candidates it was downgraded on exactly this basis). The patent angle for each entry is a screening of possible protection, not a freedom-to-operate opinion.
• The limit of the method: the independent critical-review loop is a structured adversarial review, not an expert assessment by a process chemist with a lab and a patent attorney. It lowers the risk of gross errors and catches inconsistencies, but it does not replace industry expertise before an investment decision.

The case is anonymised. The client, the specific molecules, the country and the national market are not disclosed under a confidentiality agreement; the details are for a diagnostic session under NDA. The material is informational in nature and is not investment, legal or patent advice: the patent angle is a screening, not a freedom-to-operate opinion, and before filing an application and before any investment a novelty and freedom-to-operate patent search by a patent attorney is mandatory. The figures are taken from the project report.