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Zongertinib
Tier C — Watch / tradeZongertinib
Boehringer Ingelheim International Gmbh
Originator
2025
First approval
-
Expiry (public)
No sales data
Peak sales
Small molecule
Type
Targets：HER2
Brand：HERNEXEOS
Indications (approved)：Non-small cell lung cancer
Regional status
US
Approved
2025-08-08
EU
Phase III
2024-02-09
China
Approved
2025-08-26
Japan
Approved
2025-09-19
Synthetic routes & intermediates5 routes
Originator routes × 0Optimised (non-patent) × 5Process routes × 0
Routes are ordered originator first, then optimised / process (non-patent) routes; each lists steps, overall yield and the intermediate table (code / CAS / name) — ready for supplier sourcing and RFQ. Rendered by this site from structured data; no third-party route graphics used.
OptimisedRoute 1Steps 7 · Total yield /
(I)1157260-1-a455-88-9(II)1157260-1-a,(II)1157260-1-b—(III)1157260-1-a—(IV)1157260-1-a—(Va)1157260-1-a—(Vb)1157260-1-a—(VI)1157260-1-a—(VII)1157260-1-a—(VIII)1157260-1-a73874-95-0(IX)1157260-1-a—(X)1157260-1-a—(XI)1157260-1-a814-68-6API · Zongertinib
| Code | CAS No. | Intermediate |
|---|---|---|
| (I)1157260-1-a | 455-88-9 | 1-Fluoro-2-methyl-4-nitrobenzene |
| (II)1157260-1-a,(II)1157260-1-b | - | 1-Methyl-1H-1,3-benzimidazol-5-ol |
| (III)1157260-1-a | - | 1-Methyl-5-(2-methyl-4-nitrophenoxy)-1H-1,3-benzimidazole |
| (IV)1157260-1-a | - | 3-Methyl-4-((1-methyl-1H-benzimidazol-5-yl)oxy)benzenamine |
| (Va)1157260-1-a | - | 4-Chloro-6-(methylthio)pyrimido[5,4-d]pyrimidine |
| (Vb)1157260-1-a | - | 8-Chloro-2-(methylsulfanyl)pyrimido[5,4-d]pyrimidine hydrogen chloride |
| (VI)1157260-1-a | - | N-[3-Methyl-4-[(1-methyl-1H-1,3-benzimidazol-5-yl)oxy]phenyl]-6-(methylsulfanyl)pyrimido[5,4-d]pyrimidin-4-amine |
| (VII)1157260-1-a | - | 6-(Methanesulfinyl)-N-[3-methyl-4-[(1-methyl-1H-1,3-benzimidazol-5-yl)oxy]phenyl]pyrimido[5,4-d]pyrimidin-4-amine |
| (VIII)1157260-1-a | 73874-95-0 | 1,1-Dimethylethyl piperidin-4-ylcarbamate |
| (IX)1157260-1-a | - | tert-Butyl [1-(8-[3-methyl-4-[(1-methyl-1H-1,3-benzimidazol-5-yl)oxy]anilino]pyrimido[5,4-d]pyrimidin-2-yl)piperidin-4-yl]carbamate |
| (X)1157260-1-a | - | 6-(4-Aminopiperidin-1-yl)-N-[3-methyl-4-[(1-methyl-1H-1,3-benzimidazol-5-yl)oxy]phenyl]pyrimido[5,4-d]pyrimidin-4-amine |
| (XI)1157260-1-a | 814-68-6Available | 2-Propenoyl chloride |
OptimisedRoute 2Steps 4 · Total yield /
(II)1157260-1-a,(II)1157260-1-b—(XII)1157260-1-b96-96-8(XIII)1157260-1-b74-88-4(XIV)1157260-1-b—(XV)1157260-1-b—(XVI)1157260-1-b3473-63-0(XVII)1157260-1-b—API · Zongertinib
| Code | CAS No. | Intermediate |
|---|---|---|
| (II)1157260-1-a,(II)1157260-1-b | - | 1-Methyl-1H-1,3-benzimidazol-5-ol |
| (XII)1157260-1-b | 96-96-8 | 2-Nitro-p-anisidine |
| (XIII)1157260-1-b | 74-88-4Available | Iodomethane |
| (XIV)1157260-1-b | - | 4-Methoxy-N-methyl-2-nitroaniline |
| (XV)1157260-1-b | - | 4-Methoxy-N1-methylbenzene-1,2-diamine |
| (XVI)1157260-1-b | 3473-63-0 | Aminomethylideneazanium acetate |
| (XVII)1157260-1-b | - | 5-Methoxy-1-methyl-1H-1,3-benzimidazole |
OptimisedRoute 3Steps 7 · Total yield /
(I)1157260-2-a98550-19-7(II)1157260-2-a—(III)1157260-2-a,(III)1157260-2-b—(IVa)1157260-2-a—(IVb)1157260-2-a—(V)1157260-2-a—(VI)1157260-2-a73874-95-0(VII)1157260-2-a—(VIII)1157260-2-a—(IX)1157260-2-a625-36-5(X)1157260-2-a—API · Zongertinib
| Code | CAS No. | Intermediate |
|---|---|---|
| (I)1157260-2-a | 98550-19-7 | 6-(Methylsulfanyl)-[1,3]diazino[5,4-d]pyrimidin-4-ol |
| (II)1157260-2-a | - | 4-Chloro-6-(methylthio)pyrimido[5,4-d]pyrimidine |
| (III)1157260-2-a,(III)1157260-2-b | - | 3-Methyl-4-((1-methyl-1H-benzimidazol-5-yl)oxy)benzenamine |
| (IVa)1157260-2-a | - | N-[3-Methyl-4-[(1-methyl-1H-1,3-benzimidazol-5-yl)oxy]phenyl]-6-(methylsulfanyl)pyrimido[5,4-d]pyrimidin-4-amine |
| (IVb)1157260-2-a | - | N-[3-Methyl-4-[(1-methyl-1H-1,3-benzimidazol-5-yl)oxy]phenyl]-6-(methylsulfanyl)pyrimido[5,4-d]pyrimidin-4-amine hydrogen chloride |
| (V)1157260-2-a | - | 6-(Methanesulfonyl)-N-[3-methyl-4-[(1-methyl-1H-1,3-benzimidazol-5-yl)oxy]phenyl]pyrimido[5,4-d]pyrimidin-4-amine |
| (VI)1157260-2-a | 73874-95-0 | 1,1-Dimethylethyl piperidin-4-ylcarbamate |
| (VII)1157260-2-a | - | tert-Butyl [1-(8-[3-methyl-4-[(1-methyl-1H-1,3-benzimidazol-5-yl)oxy]anilino]pyrimido[5,4-d]pyrimidin-2-yl)piperidin-4-yl]carbamate |
| (VIII)1157260-2-a | - | 6-(4-Aminopiperidin-1-yl)-N-[3-methyl-4-[(1-methyl-1H-1,3-benzimidazol-5-yl)oxy]phenyl]pyrimido[5,4-d]pyrimidin-4-amine hydrogen chloride (1/3) |
| (IX)1157260-2-a | 625-36-5Available | (Chloromethyl)acetyl chloride |
| (X)1157260-2-a | - | 3-Chloro-N-[1-(8-[3-methyl-4-[(1-methyl-1H-1,3-benzimidazol-5-yl)oxy]anilino]pyrimido[5,4-d]pyrimidin-2-yl)piperidin-4-yl]propanamide |
OptimisedRoute 4Steps 5 · Total yield /
(III)1157260-2-a,(III)1157260-2-b—(XI)1157260-2-b455-88-9(XII)1157260-2-b610-81-1(XIII)1157260-2-b—(XIV)1157260-2-b77-78-1(XV)1157260-2-b—(XVI)1157260-2-b—(XVII)1157260-2-b64-18-6(XVIII)1157260-2-b—API · Zongertinib
| Code | CAS No. | Intermediate |
|---|---|---|
| (III)1157260-2-a,(III)1157260-2-b | - | 3-Methyl-4-((1-methyl-1H-benzimidazol-5-yl)oxy)benzenamine |
| (XI)1157260-2-b | 455-88-9 | 1-Fluoro-2-methyl-4-nitrobenzene |
| (XII)1157260-2-b | 610-81-1 | 4-Amino-3-nitrophenol |
| (XIII)1157260-2-b | - | 4-(2-Methyl-4-nitrophenoxy)-2-nitroaniline |
| (XIV)1157260-2-b | 77-78-1Available | Dimethoxysulfone |
| (XV)1157260-2-b | - | N-Methyl-4-(2-methyl-4-nitrophenoxy)-2-nitroaniline |
| (XVI)1157260-2-b | - | 4-(4-Amino-2-methylphenoxy)-N1-methylbenzene-1,2-diamine |
| (XVII)1157260-2-b | 64-18-6 | Formic acid |
| (XVIII)1157260-2-b | - | N-[3-Methyl-4-[(1-methyl-1H-1,3-benzimidazol-5-yl)oxy]phenyl]formamide |
OptimisedRoute 5Steps 3 · Total yield /
(I)1157260-3-a—(II)1157260-3-a—(III)1157260-3-a—(IV)1157260-3-a—API · Zongertinib
| Code | CAS No. | Intermediate |
|---|---|---|
| (I)1157260-3-a | - | 6-(Methanesulfonyl)-N-[3-methyl-4-[(1-methyl-1H-1,3-benzimidazol-5-yl)oxy]phenyl]pyrimido[5,4-d]pyrimidin-4-amine |
| (II)1157260-3-a | - | 3-(Methylsulfanyl)-N-(piperidin-4-yl)propanamide |
| (III)1157260-3-a | - | N-[1-(8-[3-Methyl-4-[(1-methyl-1H-1,3-benzimidazol-5-yl)oxy]anilino]pyrimido[5,4-d]pyrimidin-2-yl)piperidin-4-yl]-3-(methylsulfanyl)propanamide |
| (IV)1157260-3-a | - | 3-(Methanesulfonyl)-N-[1-(8-[3-methyl-4-[(1-methyl-1H-1,3-benzimidazol-5-yl)oxy]anilino]pyrimido[5,4-d]pyrimidin-2-yl)piperidin-4-yl]propanamide |
Frequently asked questions
What are the approved indications of Zongertinib?
Approved indications include: Non-small cell lung cancer.
When does the Zongertinib patent expire?
No public expiry year is available for Zongertinib yet; this page updates once verified.
How many synthesis routes are recorded for Zongertinib?
5 synthesis routes are recorded; the shortest is 3 steps with / total yield. Intermediates in each route carry codes and CAS numbers.
Where can I buy Zongertinib intermediates?
4 intermediate CAS of Zongertinib are available through the Unibest supply network — see the route tables on this page and request a quote per CAS.
How do I get a quote for Zongertinib intermediates?
Open the CAS profile of the target intermediate from this page, or submit an RFQ directly — the CAS enters the matching flow automatically and the supply network responds with quotes.
Source: cross-verified data (structured fields only) · 2026-10-22