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普拉替尼
Tier C — Watch / tradePralsetinib · all drugs expiring in 2031 →
Blueprint Medicines Corp
Originator
2020
First approval
2031
Expiry (public)
$0.3B *
Peak sales
化学药
Type
Targets：RET
Brand：Pujihua、普吉华、GAVRETO、Gavreto
Indications (approved)：非小细胞肺癌、甲状腺瘤、甲状腺髓样癌
Regional status
US
批准上市
2020-09-04
EU
批准上市
2021-11-18
China
批准上市
2021-03-24
Japan
终止
2020-07-24
Synthetic routes & intermediates7 routes
Originator routes × 0Optimised (non-patent) × 7Process 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 8 · Total yield /
| Code | CAS No. | Intermediate |
|---|---|---|
| (I)1024528-1-a,(I)1024528-1-d | 4746-97-8 | 1,4 Cyclohexanedione ethylene ketal |
| (II)1024528-1-a | 2097133-36-1 | Methyl 8-methoxy-1,4-dioxaspiro[4.5]decane-8-carboxylate |
| (III)1024528-1-a | 1622928-67-9 | Methyl 1-methoxy-4-oxocyclohexane-1-carboxylate |
| (IV)1024528-1-a | 2097133-42-9 | Methyl 4-hydroxy-1-methoxycyclohexane-1-carboxylate |
| (V)1024528-1-a | 2097133-18-9 | Methyl 4-iodo-1-methoxycyclohexane-1-carboxylate |
| (VI)1024528-1-a | 89466-59-1 | 2-Chloro-4-methyl-6-(methylsulfanyl)pyrimidine |
| (VII)1024528-1-a | 5424-21-5 | 2,4-Dichloro-6-methylpyrimidine |
| (VIII)1024528-1-a | 2742918-71-2 | Methyl 1-methoxy-4-[4-methyl-6-(methylsulfanyl)pyrimidin-2-yl]cyclohexane-1-carboxylate |
| (IX)1024528-1-a | 2097133-29-2 | Methyl 4-[4-(methanesulfonyl)-6-methylpyrimidin-2-yl]-1-methoxycyclohexane-1-carboxylate |
| (X)1024528-1-a,(X)1024528-1-d | 2097133-30-5 | Methyl 1-methoxy-4-(4-methyl-6-oxo-1,6-dihydropyrimidin-2-yl)cyclohexane-1-carboxylate |
| (XI)1024528-1-a,(XI)1024528-1-b | 2097133-31-6 | Methyl 4-(4-chloro-6-methylpyrimidin-2-yl)-1-methoxycyclohexane-1-carboxylate |
OptimisedRoute 2Steps 4 · Total yield /
| Code | CAS No. | Intermediate |
|---|---|---|
| (XI)1024528-1-a,(XI)1024528-1-b | 2097133-31-6 | Methyl 4-(4-chloro-6-methylpyrimidin-2-yl)-1-methoxycyclohexane-1-carboxylate |
| (XII)1024528-1-b | 31230-17-8 | 3-Amino-5-methylpyrazole |
| (XIII)1024528-1-b | 2097133-32-7 | Methyl 1-methoxy-4-[4-methyl-6-[(5-methyl-1H-pyrazol-3-yl)amino]pyrimidin-2-yl]cyclohexane-1-carboxylate |
| (XIV)1024528-1-b | 2459966-45-9 | 1-Methoxy-4-[4-methyl-6-[(5-methyl-1H-pyrazol-3-yl)amino]pyrimidin-2-yl]cyclohexane-1-carboxylic acid |
| (XIX)1024528-1-b,(XIX)1024528-1-c | 1980023-94-6 | 1-[6-(4-Fluoro-1H-pyrazol-1-yl)pyridin-3-yl]ethan-1-one |
| (XV)1024528-1-b | 139042-59-4 | 1-(6-Bromopyridin-3-yl)ethan-1-one |
| (XVa)1024528-1-b | 2097133-17-8 | (1S)-1-[6-(4-Fluoro-1H-pyrazol-1-yl)pyridin-3-yl]ethan-1-amine hydrogen chloride |
| (XVb)1024528-1-b | 1980023-96-8 | (1S)-1-[6-(4-Fluoro-1H-pyrazol-1-yl)pyridin-3-yl]ethan-1-amine |
| (XVc)1024528-1-b | - | (1S)-1-[6-(4-Fluoro-1H-pyrazol-1-yl)pyridin-3-yl]ethan-1-amine hydrogen chloride (1/2) |
| (XVII)1024528-1-b,(XVII)1024528-1-c | 35277-02-2 | 4-Fluoro-1H-pyrazole |
| (XVIII)1024528-1-b | 102-52-3 | 1,1,3,3-Tetrakis(methyloxy)propane |
| (XX)1024528-1-b | 196929-78-9 | (R)-(+)-2-Methyl-2-propanesulfinamide |
| (XXI)1024528-1-b | 1980023-95-7 | (SR)-N-[(1S)-1-[6-(4-Fluoro-1H-pyrazol-1-yl)pyridin-3-yl]ethyl]-2-methylpropane-2-sulfinamide |
OptimisedRoute 3Steps 7 · Total yield /
| Code | CAS No. | Intermediate |
|---|---|---|
| (XIX)1024528-1-b,(XIX)1024528-1-c | 1980023-94-6 | 1-[6-(4-Fluoro-1H-pyrazol-1-yl)pyridin-3-yl]ethan-1-one |
| (XVII)1024528-1-b,(XVII)1024528-1-c | 35277-02-2 | 4-Fluoro-1H-pyrazole |
| (XXII)1024528-1-c | 76-37-9 | 2,2,3,3-Tetrafluoropropan-1-ol |
| (XXIII)1024528-1-c | 343331-58-8 | 4-(2,2,3,3-Tetrafluoropropyl)morpholine |
| (XXIV)1024528-1-c | 1438425-76-3 | 4-Methyl-4-(2,2,3,3-tetrafluoropropyl)morpholin-4-ium mesylate |
| (XXIX)1024528-1-c | 288-13-1Available | 1,2-Diazole |
| (XXV)1024528-1-c | - | 4-Methyl-4-[(1Z)-2,3,3-trifluoroprop-1-en-1-yl]morpholin-4-ium methanesulfonate |
| (XXVI)1024528-1-c | - | (2Z)-2-Fluoro-3-(morpholin-4-yl)prop-2-enal |
| (XXVII)1024528-1-c | 5341-61-7 | Hydrazine dihydrochloride |
| (XXVIII)1024528-1-c | - | 4-Fluoro-1H-pyrazole hydrogen chloride |
| (XXX)1024528-1-c | 53939-30-3 | 5-Bromo-2-chloropyridine |
| (XXXI)1024528-1-c | 108-24-7 | Acetic acid acetic anhydride |
| (XXXII)1024528-1-c | 55676-22-7 | 1-(6-Chloropyridin-3-yl)ethanone |
OptimisedRoute 4Steps 6 · Total yield /
| Code | CAS No. | Intermediate |
|---|---|---|
| (I)1024528-1-a,(I)1024528-1-d | 4746-97-8 | 1,4 Cyclohexanedione ethylene ketal |
| (X)1024528-1-a,(X)1024528-1-d | 2097133-30-5 | Methyl 1-methoxy-4-(4-methyl-6-oxo-1,6-dihydropyrimidin-2-yl)cyclohexane-1-carboxylate |
| (XXXIII)1024528-1-d | 69947-09-7 | 1,4-Dioxaspiro[4.5]decane-8-carbonitrile |
| (XXXIV)1024528-1-d | 1252690-12-2 | N-Hydroxy-1,4-dioxaspiro[4.5]decane-8-carboximidamide |
| (XXXV)1024528-1-d | 1252973-00-4 | 1,4-Dioxaspiro[4.5]decane-8-carboximidamide |
| (XXXVI)1024528-1-d | 141-97-9Available | 1-Ethoxybutane-1,3-dione |
| (XXXVII)1024528-1-d | - | 2-(1,4-Dioxaspiro[4.5]decan-8-yl)-6-methylpyrimidin-4-ol |
| (XXXVIII)1024528-1-d | - | 4-(4-Hydroxy-6-methylpyrimidin-2-yl)cyclohexan-1-one |
OptimisedRoute 5Steps 5 · Total yield /
| Code | CAS No. | Intermediate |
|---|---|---|
| (I)1024528-2-a | 14394-60-6 | 2-Chloro-6-methylpyrimidin-4-amine |
| (II)1024528-2-a | 2675521-17-0 | tert-Butyl (2-chloro-6-methylpyrimidin-4-yl)carbamate |
| (III)1024528-2-a | 2097133-18-9 | Methyl 4-iodo-1-methoxycyclohexane-1-carboxylate |
| (IV)1024528-2-a | 2675521-16-9 | Methyl 4-[4-[(tert-butoxycarbonyl)amino]-6-methylpyrimidin-2-yl]-1-methoxycyclohexane-1-carboxylate |
| (V)1024528-2-a | 2097133-30-5 | Methyl 1-methoxy-4-(4-methyl-6-oxo-1,6-dihydropyrimidin-2-yl)cyclohexane-1-carboxylate |
| (VI)1024528-2-a | 578008-32-9 | 3-Amino-1-Boc-5-methyl-1H-pyrazole |
| (VII)1024528-2-a | 2097133-32-7 | Methyl 1-methoxy-4-[4-methyl-6-[(5-methyl-1H-pyrazol-3-yl)amino]pyrimidin-2-yl]cyclohexane-1-carboxylate |
| (VIII)1024528-2-a | 1980023-96-8 | (1S)-1-[6-(4-Fluoro-1H-pyrazol-1-yl)pyridin-3-yl]ethan-1-amine |
OptimisedRoute 6Steps 7 · Total yield /
| Code | CAS No. | Intermediate |
|---|---|---|
| (I)1024528-3-a,(I)1024528-3-b | 2778223-41-7 | Methyl 4-cyano-1-methoxycyclohexane-1-carboxylate |
| (II)1024528-3-a | - | Methyl 4-[imino(methoxy)methyl]-1-methoxycyclohexane-1-carboxylate hydrogen chloride |
| (III)1024528-3-a | - | Methyl trans-4-carbamimidoyl-1-methoxycyclohexane-1-carboxylate |
| (IV)1024528-3-a | 105-45-3Available | 1-Methoxybutane-1,3-dione |
| (V)1024528-3-a | 2097133-30-5 | Methyl 1-methoxy-4-(4-methyl-6-oxo-1,6-dihydropyrimidin-2-yl)cyclohexane-1-carboxylate |
| (VI)1024528-3-a | - | Methyl trans-4-[4-[(methanesulfonyl)oxy]-6-methylpyrimidin-2-yl]-1-methoxycyclohexane-1-carboxylate |
| (VII)1024528-3-a | 31230-17-8 | 3-Amino-5-methylpyrazole |
| (VIII)1024528-3-a | - | Methyl (1s,4s)-1-methoxy-4-[4-methyl-6-[(5-methyl-1H-pyrazol-3-yl)amino]pyrimidin-2-yl]cyclohexane-1-carboxylate |
| (IX)1024528-3-a | - | (1s,4s)-1-Methoxy-4-[4-methyl-6-[(5-methyl-1H-pyrazol-3-yl)amino]pyrimidin-2-yl]cyclohexane-1-carboxylic acid |
| (Xa)1024528-3-a | 1980023-96-8 | (1S)-1-[6-(4-Fluoro-1H-pyrazol-1-yl)pyridin-3-yl]ethan-1-amine |
| (Xb)1024528-3-a | 2097133-17-8 | (1S)-1-[6-(4-Fluoro-1H-pyrazol-1-yl)pyridin-3-yl]ethan-1-amine hydrogen chloride |
OptimisedRoute 7Steps 3 · Total yield /
| Code | CAS No. | Intermediate |
|---|---|---|
| (I)1024528-3-a,(I)1024528-3-b | 2778223-41-7 | Methyl 4-cyano-1-methoxycyclohexane-1-carboxylate |
| (Xb)1024528-3-a | 2097133-17-8 | (1S)-1-[6-(4-Fluoro-1H-pyrazol-1-yl)pyridin-3-yl]ethan-1-amine hydrogen chloride |
| (XI)1024528-3-b | 4746-97-8 | 1,4 Cyclohexanedione ethylene ketal |
| (XII)1024528-3-b | 2097133-36-1 | Methyl 8-methoxy-1,4-dioxaspiro[4.5]decane-8-carboxylate |
| (XIII)1024528-3-b | 1622928-67-9 | Methyl 1-methoxy-4-oxocyclohexane-1-carboxylate |
| (XIV)1024528-3-b | 69947-09-7 | 1,4-Dioxaspiro[4.5]decane-8-carbonitrile |
| (XV)1024528-3-b | 34916-10-4 | 4-Oxocyclohexane-1-carbonitrile |
Frequently asked questions
What are the approved indications of Pralsetinib?
Approved indications include: 非小细胞肺癌, 甲状腺瘤, 甲状腺髓样癌.
When does the Pralsetinib patent expire?
Based on public sources, the Pralsetinib patent expires in 2031.
How many synthesis routes are recorded for Pralsetinib?
7 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 Pralsetinib intermediates?
3 intermediate CAS of Pralsetinib 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 Pralsetinib 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) · 2026-09-24