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拉考沙胺

Tier B — Position early

Lacosamide · all drugs expiring in 2028 →

比利时优时比制药有限公司
Originator
2008
First approval
2028
Expiry (public)
$1.92B ▲
Peak sales
化学药
Type

Targets：NMDAR、SCNA

Brand：Vimpat、维派特

Indications (approved)：强直阵挛性癫痫、癫痫、癫痫部分性发作、癫痫发作

Regional status

US
批准上市
2008-10-28
EU
批准上市
2008-08-29
China
批准上市
2018-11-21
Japan
批准上市
2016-07-04

Synthetic routes & intermediates7 routes

Originator routes × 1Optimised (non-patent) × 6Process 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 3 · Total yield 2 g
Synthetic routes & intermediates Route 1
CodeCAS No.Intermediate
LACO-001312-84-5D-serine
LACO-002152612-69-6acetyl-D-serine
LACO-003175481-38-6(R)-2-acetamido-N-benzyl-3-hydroxypropanamide
OptimisedRoute 2Steps 5 · Total yield 50 g
Synthetic routes & intermediates Route 2
CodeCAS No.Intermediate
LACO-001312-84-5D-serine
LACO-00476-83-5(chloromethanetriyl)tribenzene
LACO-005150094-69-2trityl-D-serine
LACO-006100-46-9Availablephenylmethanamine
LACO-0071085337-38-7(R)-N-benzyl-3-hydroxy-2-(tritylamino)propanamide
LACO-0081159573-88-2(R)-N-benzyl-3-methoxy-2-(tritylamino)propanamide
LACO-009196601-69-1(R)-2-amino-N-benzyl-3-methoxypropanamide
OptimisedRoute 3Steps 4 · Total yield 10.5 g
Synthetic routes & intermediates Route 3
CodeCAS No.Intermediate
LACO-0106368-20-3(tert-butoxycarbonyl)-D-serine
LACO-01174-88-4Availableiodomethane-11C
LACO-01286123-95-7N-(tert-butoxycarbonyl)-O-methyl-D-serine
LACO-01386118-11-8O-methyl-D-serine
LACO-014196601-67-9N-acetyl-O-methyl-D-serine
OptimisedRoute 4Steps 5 · Total yield /
Synthetic routes & intermediates Route 4
CodeCAS No.Intermediate
LACO-006100-46-9Availablephenylmethanamine
LACO-009196601-69-1(R)-2-amino-N-benzyl-3-methoxypropanamide
LACO-0153674-13-3ethyl 2,3-dibromopropanoate
LACO-016124-41-4Availablesodium methanolate
LACO-01765090-78-02-bromo-3-methoxypropanoic acid
LACO-018705283-58-5N-benzyl-2-bromo-3-methoxypropanamide
LACO-019262845-82-92-amino-N-benzyl-3-methoxypropanamide
LACO-02017026-42-5(2S,3S)-2,3-bis(benzoyloxy)succinic acid
OptimisedRoute 5Steps 6 · Total yield 95 mg
Synthetic routes & intermediates Route 5
CodeCAS No.Intermediate
LACO-006100-46-9Availablephenylmethanamine
LACO-014196601-67-9N-acetyl-O-methyl-D-serine
LACO-02124184-43-8methyl D-serinate
LACO-02218509-25-6diethoxytriphenyl-l5-phosphane
LACO-023353291-72-2ethyl (R)-aziridine-2-carboxylate
LACO-024103539-32-8methyl (R)-aziridine-2-carboxylate
LACO-0251084734-42-8ethyl (R)-1-acetylaziridine-2-carboxylate
LACO-026177473-24-4methyl (R)-1-acetylaziridine-2-carboxylate
LACO-0271084734-55-3ethyl N-acetyl-O-methyl-D-serinate
LACO-028196601-66-8methyl N-acetyl-O-methyl-D-serinate
LACO-0293945-69-54-(4,6-dimethoxy-1,3,5-triazin-2-yl)-4-methylmorpholin-4-ium chloride
LACO-030603-35-0triphenylphosphane
LACO-03180923-55-3sodium ethanolate
OptimisedRoute 6Steps 4 · Total yield 18.7 g
Synthetic routes & intermediates Route 6
CodeCAS No.Intermediate
LACO-006100-46-9Availablephenylmethanamine
LACO-009196601-69-1(R)-2-amino-N-benzyl-3-methoxypropanamide
LACO-0106368-20-3(tert-butoxycarbonyl)-D-serine
LACO-01286123-95-7N-(tert-butoxycarbonyl)-O-methyl-D-serine
LACO-032880468-89-3tert-butyl (R)-(1-(benzylamino)-3-methoxy-1-oxopropan-2-yl)carbamate
OptimisedRoute 7Steps 3 · Total yield 621 mg (Lacosamide)
Synthetic routes & intermediates Route 7
CodeCAS No.Intermediate
LACO-03368820-71-3ethyl (R)-1-((S)-1-phenylethyl)aziridine-2-carboxylate
LACO-0342051583-26-5ethyl O-methyl-N-((S)-1-phenylethyl)-D-serinate
LACO-0271084734-55-3ethyl N-acetyl-O-methyl-D-serinate
Lacosamide175481-36-4(R)-2-acetamido-N-benzyl-3-methoxypropionamide

Frequently asked questions

What are the approved indications of Lacosamide?

Approved indications include: 强直阵挛性癫痫, 癫痫, 癫痫部分性发作, 癫痫发作.

When does the Lacosamide patent expire?

Based on public sources, the Lacosamide patent expires in 2028.

How many synthesis routes are recorded for Lacosamide?

7 synthesis routes are recorded; the shortest is 3 steps with 2 g total yield. Intermediates in each route carry codes and CAS numbers.

Where can I buy Lacosamide intermediates?

3 intermediate CAS of Lacosamide 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 Lacosamide 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