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洛拉替尼

Tier B — Position early

Lorlatinib · all drugs expiring in 2030 →

辉瑞
Originator
2018
First approval
2030
Expiry (public)
$1.02B ▲
Peak sales
化学药
Type

TargetsALK、ROS

BrandLorbrena、博瑞纳、Lorviqua

Indications (approved)非小细胞肺癌

Regional status

US
批准上市
2018-11-02
EU
批准上市
2019-05-06
China
批准上市
2022-04-27
Japan
批准上市
2018-09-21

Synthetic routes & intermediates2 routes

Originator routes × 1Optimised (non-patent) × 1Process 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.

OriginatorRoute 1Steps 9 · Total yield 110 mg
Synthetic routes & intermediates Route 1
CodeCAS No.Intermediate
LORL-001914225-70-01-(5-fluoro-2-iodophenyl)ethanone
LORL-0021454847-96-1(S)-1-(5-fluoro-2-iodophenyl)ethanol
LORL-0031454847-97-2(S)-1-(5-fluoro-2-iodophenyl)ethyl methanesulfonate
LORL-00416867-03-12-aminopyridin-3-ol
LORL-0051454847-98-3(R)-3-(1-(5-fluoro-2-iodophenyl)ethoxy)pyridin-2-amine
LORL-0061454847-99-4(R)-methyl 2-(1-((2-aminopyridin-3-yl)oxy)ethyl)-4-fluorobenzoate
LORL-0071454848-00-0(R)-methyl 2-(1-((2-amino-5-bromopyridin-3-yl)oxy)ethyl)-4-fluorobenzoate
LORL-0081454848-24-8tert-butyl ((4-bromo-5-cyano-1-methyl-1H-pyrazol-3-yl)methyl)(methyl)carbamate
LORL-009-(R)-methyl 2-(1-((2-amino-5-(3-(((tert-butoxycarbonyl)(methyl)amino)methyl)-5-cyano-1-methyl-1H-pyrazol-4-yl)pyridin-3-yl)oxy)ethyl)-4-fluorobenzoate
LORL-010-(R)-2-(1-((2-amino-5-(3-(((tert-butoxycarbonyl)(methyl)amino)methyl)-5-cyano-1-methyl-1H-pyrazol-4-yl)pyridin-3-yl)oxy)ethyl)-4-fluorobenzoic acid
LORL-0111454850-15-7(R)-2-(1-((2-amino-5-(5-cyano-1-methyl-3-((methylamino)methyl)-1H-pyrazol-4-yl)pyridin-3-yl)oxy)ethyl)-4-fluorobenzoic acid hydrochloride
OptimisedRoute 2Steps 11 · Total yield 2.25 g
Synthetic routes & intermediates Route 2
CodeCAS No.Intermediate
LORL-0051454847-98-3(R)-3-(1-(5-fluoro-2-iodophenyl)ethoxy)pyridin-2-amine
LORL-0081454848-24-8tert-butyl ((4-bromo-5-cyano-1-methyl-1H-pyrazol-3-yl)methyl)(methyl)carbamate
LORL-0125775-89-3ethyl 4-bromo-1,3-dimethyl-1H-pyrazole-5-carboxylate
LORL-0131454848-19-1ethyl 4-bromo-3-(bromomethyl)-1-methyl-1H-pyrazole-5-carboxylate
LORL-01416066-84-5tert-butyl methylcarbamate
LORL-0151454848-21-5ethyl 4-bromo-3-(((tert-butoxycarbonyl)(methyl)amino)methyl)-1-methyl-1H-pyrazole-5-carboxylate
LORL-0161454848-22-64-bromo-3-(((tert-butoxycarbonyl)(methyl)amino)methyl)-1-methyl-1H-pyrazole-5-carboxylic acid
LORL-0171454848-23-7tert-butyl ((4-bromo-5-carbamoyl-1-methyl-1H-pyrazol-3-yl)methyl)(methyl)carbamate
LORL-0181454848-70-4tert-butyl ((5-cyano-1-methyl-1H-pyrazol-3-yl)methyl)(methyl)carbamate
LORL-0191454852-76-61-methyl-3-((methylamino)methyl)-1H-pyrazole-5-carbonitrile
LORL-0201612891-02-7(R)-2-(1-((2-aminopyridin-3-yl)oxy)ethyl)-N-((5-cyano-1-methyl-1H-pyrazol-3-yl)methyl)-4-fluoro-N-methylbenzamide
LORL-0211612891-03-8(R)-2-(1-((2-amino-5-bromopyridin-3-yl)oxy)ethyl)-N-((5-cyano-1-methyl-1H-pyrazol-3-yl)methyl)-4-fluoro-N-methylbenzamide
LORL-0221612891-04-9(R)-2-(1-((2-(N-acetylacetamido)-5-bromopyridin-3-yl)oxy)ethyl)-N-((5-cyano-1-methyl-1H-pyrazol-3-yl)methyl)-4-fluoro-N-methylbenzamide

Frequently asked questions

What are the approved indications of Lorlatinib?

Approved indications include: 非小细胞肺癌.

When does the Lorlatinib patent expire?

Based on public sources, the Lorlatinib patent expires in 2030.

How many synthesis routes are recorded for Lorlatinib?

2 synthesis routes are recorded; the shortest is 9 steps with 110 mg total yield. Intermediates in each route carry codes and CAS numbers.

Where can I buy Lorlatinib intermediates?

All intermediates in Lorlatinib 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 Lorlatinib 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