← Back to patent-cliff list
Berotralstat
Tier C — Watch / tradeBerotralstat
Biocryst Pharmaceuticals Inc
Originator
2020
First approval
-
Expiry (public)
$0.01B ▲
Peak sales
Small molecule
Type
Targets：KLKB1
Brand：ORLADEYO
Indications (approved)：遗传性血管性水肿
Regional status
US
Approved
2020-12-03
EU
Approved
2021-04-30
China
-
Japan
Approved
2021-01-22
Synthetic routes & intermediates4 routes
Originator routes × 0Optimised (non-patent) × 2Process routes × 2
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 6 · Total yield /
Berotralstat-0011809015-69-7Berotralstat-002—Berotralstat-0031809015-77-7Berotralstat-004640287-99-6Berotralstat-0051809015-78-8Berotralstat-006—Berotralstat-0071809015-79-9Berotralstat-0081809010-16-9Berotralstat-0091809010-50-1API · Berotralstat
| Code | CAS No. | Intermediate |
|---|---|---|
| Berotralstat-001 | 1809015-69-7 | [3-[Bis(trimethylsilyl)amino]-4-fluorophenyl](bromido)magnesium |
| Berotralstat-002 | - | 3-Formylbenzonitrile |
| Berotralstat-003 | 1809015-77-7 | 3-[(3-Amino-4-fluorophenyl)(hydroxy)methyl]benzonitrile |
| Berotralstat-004 | 640287-99-6 | 1-(3-[[(tert-Butoxycarbonyl)amino]methyl]phenyl)-3-(trifluoromethyl)-1H-pyrazole-5-carboxylic acid |
| Berotralstat-005 | 1809015-78-8 | tert-Butyl ([3-[5-([5-[(3-cyanophenyl)(hydroxy)methyl]-2-fluorophenyl]carbamoyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl]phenyl]methyl)carbamate |
| Berotralstat-006 | - | Cyclopropylmethanamine |
| Berotralstat-007 | 1809015-79-9 | tert-Butyl [(3-[5-[(5-[(3-cyanophenyl)[(cyclopropylmethyl)amino]methyl]-2-fluorophenyl)carbamoyl]-3-(trifluoromethyl)-1H-pyrazol-1-yl]phenyl)methyl]carbamate |
| Berotralstat-008 | 1809010-16-9 | 1-[3-(Aminomethyl)phenyl]-N-(5-[(3-cyanophenyl)[(cyclopropylmethyl)amino]methyl]-2-fluorophenyl)-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide |
| Berotralstat-009 | 1809010-50-1 | 1-[3-(Aminomethyl)phenyl]-N-(5-[(R)-(3-cyanophenyl)[(cyclopropylmethyl)amino]methyl]-2-fluorophenyl)-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide |
OptimisedRoute 2Steps 4 · Total yield /
Berotralstat-004640287-99-6Berotralstat-010—Berotralstat-011326-90-9Berotralstat-012284463-59-8Berotralstat-013209917-93-1Berotralstat-014640287-98-5API · Berotralstat
| Code | CAS No. | Intermediate |
|---|---|---|
| Berotralstat-004 | 640287-99-6 | 1-(3-[[(tert-Butoxycarbonyl)amino]methyl]phenyl)-3-(trifluoromethyl)-1H-pyrazole-5-carboxylic acid |
| Berotralstat-010 | - | 3-aminobenzonitrile |
| Berotralstat-011 | 326-90-9 | 4,4,4-trifluoro-1-(furan-2-yl)butane-1,3-dione |
| Berotralstat-012 | 284463-59-8 | 3-[5-(Furan-2-yl)-3-(trifluoromethyl)-1H-pyrazol-1-yl]benzonitrile |
| Berotralstat-013 | 209917-93-1 | 1-(3-Cyanophenyl)-3-(trifluoromethyl)-1H-pyrazole-5-carboxylic acid |
| Berotralstat-014 | 640287-98-5 | 1-[3-(Aminomethyl)phenyl]-3-(trifluoromethyl)-1H-pyrazole-5-carboxylic acid |
ProcessRoute 3Steps 7 · Total yield /
Berotralstat-015—Berotralstat-0161809015-68-6Berotralstat-0011809015-69-7Berotralstat-002—Berotralstat-017820971-62-8Berotralstat-0181809020-38-9Berotralstat-0192602377-06-8Berotralstat-020—Berotralstat-0212602377-11-5Berotralstat-004640287-99-6Berotralstat-0222602377-16-0API · Berotralstat
| Code | CAS No. | Intermediate |
|---|---|---|
| Berotralstat-015 | - | 5-Bromo-2-fluoroaniline |
| Berotralstat-016 | 1809015-68-6 | N-(5-Bromo-2-fluorophenyl)-1,1,1-trimethyl-N-(trimethylsilyl)silanamine |
| Berotralstat-001 | 1809015-69-7 | [3-[Bis(trimethylsilyl)amino]-4-fluorophenyl](bromido)magnesium |
| Berotralstat-002 | - | 3-Formylbenzonitrile |
| Berotralstat-017 | 820971-62-8 | (SR)-N-[(3-Cyanophenyl)methylidene]-2-methylpropane-2-sulfinamide |
| Berotralstat-018 | 1809020-38-9 | (SR)-N-[(R)-(3-Amino-4-fluorophenyl)(3-cyanophenyl)methyl]-2-methylpropane-2-sulfinamide |
| Berotralstat-019 | 2602377-06-8 | 3-[(R)-Amino(3-amino-4-fluorophenyl)methyl]benzonitrile hydrogen chloride |
| Berotralstat-020 | - | Cyclopropanal |
| Berotralstat-021 | 2602377-11-5 | Oxalic acid 3-[(R)-(3-amino-4-fluorophenyl)[(cyclopropylmethyl)amino]methyl]benzonitrile |
| Berotralstat-004 | 640287-99-6 | 1-(3-[[(tert-Butoxycarbonyl)amino]methyl]phenyl)-3-(trifluoromethyl)-1H-pyrazole-5-carboxylic acid |
| Berotralstat-022 | 2602377-16-0 | tert-Butyl [(3-[5-[(5-[(R)-(3-cyanophenyl)[(cyclopropylmethyl)amino]methyl]-2-fluorophenyl)carbamoyl]-3-(trifluoromethyl)-1H-pyrazol-1-yl]phenyl)methyl]carbamate |
ProcessRoute 4Steps 2 · Total yield /
Berotralstat-0222602377-16-0Berotralstat-0091809010-50-1API · Berotralstat
| Code | CAS No. | Intermediate |
|---|---|---|
| Berotralstat-022 | 2602377-16-0 | tert-Butyl [(3-[5-[(5-[(R)-(3-cyanophenyl)[(cyclopropylmethyl)amino]methyl]-2-fluorophenyl)carbamoyl]-3-(trifluoromethyl)-1H-pyrazol-1-yl]phenyl)methyl]carbamate |
| Berotralstat-009 | 1809010-50-1 | 1-[3-(Aminomethyl)phenyl]-N-(5-[(R)-(3-cyanophenyl)[(cyclopropylmethyl)amino]methyl]-2-fluorophenyl)-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide |
Frequently asked questions
What are the approved indications of Berotralstat?
Approved indications include: 遗传性血管性水肿.
When does the Berotralstat patent expire?
No public expiry year is available for Berotralstat yet; this page updates once verified.
How many synthesis routes are recorded for Berotralstat?
4 synthesis routes are recorded; the shortest is 2 steps with / total yield. Intermediates in each route carry codes and CAS numbers.
Where can I buy Berotralstat intermediates?
All intermediates in Berotralstat routes have CAS profiles — you can submit an RFQ per CAS and it enters the Unibest matching pool.
How do I get a quote for Berotralstat 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