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Fulzerasib
Tier C — Watch / tradeFulzerasib
-
Originator
2024
First approval
-
Expiry (public)
No sales data
Peak sales
Small molecule
Type
Targets：KRAS G12C
Brand：Dupert
Indications (approved)：Non-small cell lung cancer
Regional status
US
Phase III
2024-04-19
EU
Phase II
2023-04-25
China
Approved
2024-08-20
Japan
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Synthetic routes & intermediates4 routes
Originator routes × 0Optimised (non-patent) × 4Process 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)1225102-1-a—(II)1225102-1-a—(III)1225102-1-a—(IV)1225102-1-a78495-63-3(V)1225102-1-a—(VI)1225102-1-a—(VII)1225102-1-a438631-77-7(VIII)1225102-1-a—(IX)1225102-1-a—(X)1225102-1-a74-88-4(XI)1225102-1-a,(XI)1225102-1-b—API · Fulzerasib
| Code | CAS No. | Intermediate |
|---|---|---|
| (I)1225102-1-a | - | 6,7-Dichloro-1,2-dihydro-4-hydroxy-1-[4-methyl-2-(1-methylethyl)-3-pyridinyl]-2-oxo-1,8-naphthyridine-3-carbonitrile |
| (II)1225102-1-a | - | 6,7-Dichloro-4-hydroxy-1-(2-isopropyl-4-methyl-3-pyridyl)-1,8-naphthyridin-2-one |
| (III)1225102-1-a | - | 6,7-Dichloro-4-hydroxy-1-[4-methyl-2-(propan-2-yl)pyridin-3-yl]-3-nitro-1,8-naphthyridin-2(1H)-one |
| (IV)1225102-1-a | 78495-63-3Available | (2-Fluoro-6-methoxyphenyl)boronic acid |
| (V)1225102-1-a | - | 6-Chloro-7-(2-fluoro-6-methoxyphenyl)-4-hydroxy-1-[4-methyl-2-(propan-2-yl)pyridin-3-yl]-3-nitro-1,8-naphthyridin-2(1H)-one |
| (VI)1225102-1-a | - | 4,6-Dichloro-7-(2-fluoro-6-methoxyphenyl)-1-[4-methyl-2-(propan-2-yl)pyridin-3-yl]-3-nitro-1,8-naphthyridin-2(1H)-one |
| (VII)1225102-1-a | 438631-77-7 | (R)-Piperazine-1,3-dicarboxylic acid 1-tert-butyl 3-methyl diester |
| (VIII)1225102-1-a | - | 1-tert-Butyl 3-methyl (3R)-4-[6-chloro-7-(2-fluoro-6-methoxyphenyl)-1-[4-methyl-2-(propan-2-yl)pyridin-3-yl]-3-nitro-2-oxo-1,2-dihydro-1,8-naphthyridin-4-yl]piperazine-1,3-dicarboxylate |
| (IX)1225102-1-a | - | tert-Butyl (4aR)-11-chloro-10-(2-fluoro-6-methoxyphenyl)-8-[4-methyl-2-(propan-2-yl)pyridin-3-yl]-5,7-dioxo-1,2,4,4a,5,6,7,8-octahydro-3H-pyrazino[1',2':4,5]pyrazino[2,3-c][1,8]naphthyridine-3-carboxylate |
| (X)1225102-1-a | 74-88-4Available | Iodomethane |
| (XI)1225102-1-a,(XI)1225102-1-b | - | tert-Butyl (4aR)-11-chloro-10-(2-fluoro-6-methoxyphenyl)-6-methyl-8-[4-methyl-2-(propan-2-yl)pyridin-3-yl]-5,7-dioxo-1,2,4,4a,5,6,7,8-octahydro-3H-pyrazino[1',2':4,5]pyrazino[2,3-c][1,8]naphthyridine-3-carboxylate |
OptimisedRoute 2Steps 4 · Total yield /
(XI)1225102-1-a,(XI)1225102-1-b—(XII)1225102-1-b—(XIII)1225102-1-b814-68-6(XIV)1225102-1-b—API · Fulzerasib
| Code | CAS No. | Intermediate |
|---|---|---|
| (XI)1225102-1-a,(XI)1225102-1-b | - | tert-Butyl (4aR)-11-chloro-10-(2-fluoro-6-methoxyphenyl)-6-methyl-8-[4-methyl-2-(propan-2-yl)pyridin-3-yl]-5,7-dioxo-1,2,4,4a,5,6,7,8-octahydro-3H-pyrazino[1',2':4,5]pyrazino[2,3-c][1,8]naphthyridine-3-carboxylate |
| (XII)1225102-1-b | - | (4aR)-11-Chloro-10-(2-fluoro-6-methoxyphenyl)-6-methyl-8-[4-methyl-2-(propan-2-yl)pyridin-3-yl]-2,3,4,4a,6,8-hexahydro-1H-pyrazino[1',2':4,5]pyrazino[2,3-c][1,8]naphthyridine-5,7-dione |
| (XIII)1225102-1-b | 814-68-6Available | 2-Propenoyl chloride |
| (XIV)1225102-1-b | - | (4aR)-11-Chloro-10-(2-fluoro-6-methoxyphenyl)-6-methyl-8-[4-methyl-2-(propan-2-yl)pyridin-3-yl]-3-(prop-2-enoyl)-2,3,4,4a,6,8-hexahydro-1H-pyrazino[1',2':4,5]pyrazino[2,3-c][1,8]naphthyridine-5,7-dione |
OptimisedRoute 3Steps 5 · Total yield /
(I)1225102-2-a38496-18-3(II)1225102-2-a1698293-93-4(III)1225102-2-a—(IV)1225102-2-a—(V)1225102-2-a—(VI)1225102-2-a—(VII)1225102-2-a127852-28-2(VIII)1225102-2-a2033-24-1(IX)1225102-2-a—(X)1225102-2-a1445-91-6(XIa)1225102-2-a—(XIb)1225102-2-a—(XII)1225102-2-a,(XII)1225102-2-b—(XIII)1225102-2-a—(XIV)1225102-2-a2216-51-5(XV)1225102-2-a—API · Fulzerasib
| Code | CAS No. | Intermediate |
|---|---|---|
| (I)1225102-2-a | 38496-18-3 | 2,6-Dichloronicotinic acid |
| (II)1225102-2-a | 1698293-93-4Available | 2-Isopropyl-4-methylpyridin-3-amine |
| (III)1225102-2-a | - | 6-Chloro-2-[(2-isopropyl-4-methyl-3-pyridyl)amino]pyridine-3-carboxylic acid |
| (IV)1225102-2-a | - | 5,6-Dichloro-2-[(2-isopropyl-4-methyl-3-pyridyl)amino]pyridine-3-carboxylic acid |
| (V)1225102-2-a | - | 5,6-Dichloro-2-[[4-methyl-2-(propan-2-yl)pyridin-3-yl]amino]pyridine-3-carbonyl chloride |
| (VI)1225102-2-a | - | 3-[(1R)-1-[3,5-Bis(trifluoromethyl)phenyl]ethoxy]-3-oxopropanoic acid |
| (VII)1225102-2-a | 127852-28-2 | (alphaR)-alpha-Methyl-3,5-bis(trifluoromethyl)benzenemethanol |
| (VIII)1225102-2-a | 2033-24-1 | 2,2-Dimethyl-1,3-dioxane-4,6-dione |
| (IX)1225102-2-a | - | 3-Oxo-3-[(1S)-1-phenylethoxy]propanoic acid |
| (X)1225102-2-a | 1445-91-6 | (1S)-Methyl phenyl carbinol |
| (XIa)1225102-2-a | - | (1S)-1-[3,5-Bis(trifluoromethyl)phenyl]ethyl 3-(5,6-dichloro-2-[[4-methyl-2-(propan-2-yl)pyridin-3-yl]amino]pyridin-3-yl)-3-oxopropanoate |
| (XIb)1225102-2-a | - | (1S)-1-Phenylethyl 3-(5,6-dichloro-2-[[4-methyl-2-(propan-2-yl)pyridin-3-yl]amino]pyridin-3-yl)-3-oxopropanoate |
| (XII)1225102-2-a,(XII)1225102-2-b | - | 6,7-Dichloro-4-hydroxy-1-(2-isopropyl-4-methyl-3-pyridyl)-1,8-naphthyridin-2-one |
| (XIII)1225102-2-a | - | 3-[(1R,2S,5R)-2-Isopropyl-5-methylcyclohexoxy]-3-oxo-propanoic acid |
| (XIV)1225102-2-a | 2216-51-5 | (-)-(1R-(1-alpha,2-beta,5-alpha))-5-Methyl-2-(1-methylethyl)cyclohexanol |
| (XV)1225102-2-a | - | (1R,2S,5R)-5-Methyl-2-(propan-2-yl)cyclohexyl 3-(5,6-dichloro-2-[[4-methyl-2-(propan-2-yl)pyridin-3-yl]amino]pyridin-3-yl)-3-oxopropanoate |
OptimisedRoute 4Steps 9 · Total yield /
(aR)-(XVI)1225102-2-b—(XII)1225102-2-a,(XII)1225102-2-b—(XIX)1225102-2-b438631-77-7(XVII)1225102-2-b—(XVIII)1225102-2-b—(XX)1225102-2-b—(XXI)1225102-2-b—(XXII)1225102-2-b77-78-1(XXIII)1225102-2-b—(XXIV)1225102-2-b1256345-60-4(XXV)1225102-2-b—(XXVI)1225102-2-b—(XXVII)1225102-2-b814-68-6API · Fulzerasib
| Code | CAS No. | Intermediate |
|---|---|---|
| (aR)-(XVI)1225102-2-b | - | (aR)-6,7-Dichloro-4-hydroxy-1-(2-isopropyl-4-methyl-3-pyridyl)-1,8-naphthyridin-2-one |
| (XII)1225102-2-a,(XII)1225102-2-b | - | 6,7-Dichloro-4-hydroxy-1-(2-isopropyl-4-methyl-3-pyridyl)-1,8-naphthyridin-2-one |
| (XIX)1225102-2-b | 438631-77-7 | (R)-Piperazine-1,3-dicarboxylic acid 1-tert-butyl 3-methyl diester |
| (XVII)1225102-2-b | - | (aR)-6,7-Dichloro-4-hydroxy-1-(2-isopropyl-4-methyl-3-pyridyl)-3-nitro-1,8-naphthyridin-2-one |
| (XVIII)1225102-2-b | - | (aR)-6,7-Dichloro-1-[4-methyl-2-(propan-2-yl)pyridin-3-yl]-3-nitro-2-oxo-1,2-dihydro-1,8-naphthyridin-4-yl trifluoromethanesulfonate |
| (XX)1225102-2-b | - | (aR)-1-tert-Butyl 3-methyl (3R)-4-[6,7-dichloro-1-[4-methyl-2-(propan-2-yl)pyridin-3-yl]-3-nitro-2-oxo-1,2-dihydro-1,8-naphthyridin-4-yl]piperazine-1,3-dicarboxylate |
| (XXI)1225102-2-b | - | (aR)-tert-Butyl (4aR)-10,11-dichloro-8-[4-methyl-2-(propan-2-yl)pyridin-3-yl]-5,7-dioxo-1,2,4,4a,5,6,7,8-octahydro-3H-pyrazino[1',2':4,5]pyrazino[2,3-c][1,8]naphthyridine-3-carboxylate |
| (XXII)1225102-2-b | 77-78-1Available | Dimethoxysulfone |
| (XXIII)1225102-2-b | - | (aR)-tert-Butyl (4aR)-10,11-dichloro-6-methyl-8-[4-methyl-2-(propan-2-yl)pyridin-3-yl]-5,7-dioxo-1,2,4,4a,5,6,7,8-octahydro-3H-pyrazino[1',2':4,5]pyrazino[2,3-c][1,8]naphthyridine-3-carboxylate |
| (XXIV)1225102-2-b | 1256345-60-4Available | (2-Fluoro-6-hydroxyphenyl)boronic acid |
| (XXV)1225102-2-b | - | (aR)-tert-Butyl (4aR)-11-chloro-10-(2-fluoro-6-hydroxyphenyl)-6-methyl-8-[4-methyl-2-(propan-2-yl)pyridin-3-yl]-5,7-dioxo-1,2,4,4a,5,6,7,8-octahydro-3H-pyrazino[1',2':4,5]pyrazino[2,3-c][1,8]naphthyridine-3-carboxylate |
| (XXVI)1225102-2-b | - | (aR)-(4aR)-11-Chloro-10-(2-fluoro-6-hydroxyphenyl)-6-methyl-8-[4-methyl-2-(propan-2-yl)pyridin-3-yl]-2,3,4,4a,6,8-hexahydro-1H-pyrazino[1',2':4,5]pyrazino[2,3-c][1,8]naphthyridine-5,7-dione |
| (XXVII)1225102-2-b | 814-68-6Available | 2-Propenoyl chloride |
Frequently asked questions
What are the approved indications of Fulzerasib?
Approved indications include: Non-small cell lung cancer.
When does the Fulzerasib patent expire?
No public expiry year is available for Fulzerasib yet; this page updates once verified.
How many synthesis routes are recorded for Fulzerasib?
4 synthesis routes are recorded; the shortest is 4 steps with / total yield. Intermediates in each route carry codes and CAS numbers.
Where can I buy Fulzerasib intermediates?
6 intermediate CAS of Fulzerasib 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 Fulzerasib 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) · 2026-09-29