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Pregabalin

Tier B — Position early

Pregabalin

Pfizer Inc.
Originator
2004
First approval
-
Expiry (public)
$5.36B ▲
Peak sales
Small molecule
Type

Targets:CACNA2D1

Brand:Regabatin, Lyrica

Indications (approved):Fibromyalgia, Seizure, Postherpetic neuralgia, 神经痛, Partial-onset seizure, Diabetic neuropathy, Epilepsy, Anxiety disorder

Regional status

US
Approved
2004-12-30
EU
Approved
2004-07-05
China
Approved
2010-05-07
Japan
Approved
2010-04-16

Factories producing this API2

Factories registered as producing this API in our sourcing network (RFQ records + product master), sorted by RFQ activity; the snapshot carries no cost or customer data.

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Synthetic routes & intermediates5 routes

Originator routes × 1Optimised (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.

OriginatorRoute 1Steps 8 · Total yield /
PREG-001646-07-1PREG-00238136-29-7PREG-00396021-65-7PREG-004134458-52-9PREG-0055437-45-6PREG-006156048-93-0PREG-007156048-94-1PREG-008156048-95-2PREG-009156048-96-3PREG-010156048-97-4API · Pregabalin
CodeCAS No.Intermediate
PREG-001646-07-14-methylpentanoic acid
PREG-00238136-29-74-methylpentanoyl chloride
PREG-00396021-65-7lithium (4R,5S)-4-methyl-2-oxo-5-phenyloxazolidin-3-ide
PREG-004134458-52-9(4R,5S)-4-methyl-3-(4-methylpentanoyl)-5-phenyloxazolidin-2-one
PREG-0055437-45-6benzyl 2-bromoacetate
PREG-006156048-93-0benzyl (S)-5-methyl-3-((4R,5S)-4-methyl-2-oxo-5-phenyloxazolidine-3-carbonyl)hexanoate
PREG-007156048-94-1(S)-2-(2-(benzyloxy)-2-oxoethyl)-4-methylpentanoic acid
PREG-008156048-95-2benzyl (S)-3-(hydroxymethyl)-5-methylhexanoate
PREG-009156048-96-3benzyl (S)-5-methyl-3-((tosyloxy)methyl)hexanoate
PREG-010156048-97-4benzyl (S)-3-(azidomethyl)-5-methylhexanoate
OptimisedRoute 3Steps 5 · Total yield 12 g
PREG-011590-86-3PREG-015128013-69-4PREG-017105-56-6PREG-018294885-98-6PREG-01975143-89-4PREG-020916982-10-0API · Pregabalin
CodeCAS No.Intermediate
PREG-011590-86-33-methylbutanal
PREG-015128013-69-43-(aminomethyl)-5-methylhexanoic acid
PREG-017105-56-6Availableethyl 2-cyanoacetate
PREG-018294885-98-6diethyl 3-isobutylpentanedioate
PREG-01975143-89-43-isobutylpentanedioic acid
PREG-020916982-10-04-isobutylpiperidine-2,6-dione
OptimisedRoute 5Steps 9 · Total yield 44.6 g
PREG-02461-90-5PREG-02528659-87-2PREG-026927828-01-1PREG-027—PREG-028—PREG-029172796-26-8PREG-030—PREG-031951792-40-8PREG-032157422-27-0API · Pregabalin
CodeCAS No.Intermediate
PREG-02461-90-5(S)-2-amino-4-methylpentanoic acid
PREG-02528659-87-2(S)-2-bromo-4-methylpentanoic acid
PREG-026927828-01-1tert-butyl (S)-2-bromo-4-methylpentanoate
PREG-027-2-(tert-butyl) 1,1-diethyl (S)-4-methylpentane-1,1,2-tricarboxylate
PREG-028-(S)-2-(1,3-diethoxy-1,3-dioxopropan-2-yl)-4-methylpentanoic acid
PREG-029172796-26-8(S)-4-isobutyldihydrofuran-2(3H)-one
PREG-030-ethyl (S)-3-(iodomethyl)-5-methylhexanoate
PREG-031951792-40-8ethyl (S)-3-(azidomethyl)-5-methylhexanoate
PREG-032157422-27-0(S)-3-(azidomethyl)-5-methylhexanoic acid
ProcessRoute 2Steps 5 · Total yield 7.4 kg
PREG-011590-86-3PREG-012105-53-3PREG-01351615-30-6PREG-014186038-82-4PREG-015128013-69-4PREG-016185815-62-7API · Pregabalin
CodeCAS No.Intermediate
PREG-011590-86-33-methylbutanal
PREG-012105-53-3Availablediethyl malonate
PREG-01351615-30-6diethyl 2-(3-methylbutylidene)malonate
PREG-014186038-82-4diethyl 2-(1-cyano-3-methylbutyl)malonate
PREG-015128013-69-43-(aminomethyl)-5-methylhexanoic acid
PREG-016185815-62-7(S)-2-(carboxymethyl)-4-methylpentan-1-aminium (S)-2-hydroxy-2-phenylacetate
ProcessRoute 4Steps 4 · Total yield 1431 kg
PREG-014186038-82-4PREG-021—PREG-022181289-39-4PREG-023350801-73-9API · Pregabalin
CodeCAS No.Intermediate
PREG-014186038-82-4diethyl 2-(1-cyano-3-methylbutyl)malonate
PREG-021-sodium (3S)-3-cyano-2-(ethoxycarbonyl)-5-methylhexanoate
PREG-022181289-39-4ethyl (S)-3-cyano-5-methylhexanoate
PREG-023350801-73-9potassium (S)-3-cyano-5-methylhexanoate

Frequently asked questions

What are the approved indications of Pregabalin?

Approved indications include: Fibromyalgia, Seizure, Postherpetic neuralgia, 神经痛, Partial-onset seizure, Diabetic neuropathy, Epilepsy, Anxiety disorder.

When does the Pregabalin patent expire?

No public expiry year is available for Pregabalin yet; this page updates once verified.

How many synthesis routes are recorded for Pregabalin?

5 synthesis routes are recorded; the shortest is 4 steps with 1431 kg total yield. Intermediates in each route carry codes and CAS numbers.

Where can I buy Pregabalin intermediates?

2 intermediate CAS of Pregabalin 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 Pregabalin 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