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Apremilast

Tier B — Position early

Apremilast · all drugs expiring in 2028 →

Celgene Corporation
Originator
2014
First approval
2028
Expiry (public)
$2.29B ▲
Peak sales
Small molecule
Type

Targets:PDE4

Brand:Otezla

Indications (approved):Plaque psoriasis, Behçet's syndrome, Oral ulcer, Psoriasis, Psoriatic arthritis

Regional status

US
Approved
2014-03-21
EU
Approved
2015-01-15
China
Approved
2021-08-12
Japan
Approved
2016-12-19

Factories producing this API1

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 & intermediates6 routes

Originator routes × 1Optimised (non-patent) × 5Process 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 5 · Total yield 19.4 g
Synthetic routes & intermediates Route 1
CodeCAS No.Intermediate
APER-0011131-52-83-ethoxy-4-methoxybenzaldehyde
APER-002253168-94-41-(3-ethoxy-4-methoxyphenyl)-2-(methylsulfonyl)ethan-1-amine
APER-0031188-21-2(2S)-2-acetamido-4-methylpentanoic acid
APER-004608141-43-1(S)-1-(3-ethoxy-4-methoxyphenyl)-2-(methylsulfonyl)ethanamine (S)-2-acetamido-4-methylpentanoate
APER-0056296-53-3N-(1,3-dioxo-1,3-dihydroisobenzofuran-4-yl)acetamide
APER-006603-11-23-nitrophthalic acid
APER-0075434-20-83-aminophthalic acid
OptimisedRoute 2Steps 6 · Total yield 0.14 g
Synthetic routes & intermediates Route 2
CodeCAS No.Intermediate
APER-0011131-52-83-ethoxy-4-methoxybenzaldehyde
APER-002253168-94-41-(3-ethoxy-4-methoxyphenyl)-2-(methylsulfonyl)ethan-1-amine
APER-006603-11-23-nitrophthalic acid
APER-00860758-86-33-ethoxy-4-methoxybenzonitrile
APER-009641-70-34-nitroisobenzofuran-1,3-dione
APER-010253168-82-02-(1-(3-ethoxy-4-methoxyphenyl)-2-(methylsulfonyl)ethyl)-4-nitroisoindoline-1,3-dione
APER-011253168-83-14-amino-2-(1-(3-ethoxy-4-methoxyphenyl)-2-(methylsulfonyl)ethyl)isoindoline-1,3-dione
OptimisedRoute 3Steps 4 · Total yield 0.6 g
Synthetic routes & intermediates Route 3
CodeCAS No.Intermediate
APER-0011131-52-83-ethoxy-4-methoxybenzaldehyde
APER-0056296-53-3N-(1,3-dioxo-1,3-dihydroisobenzofuran-4-yl)acetamide
APER-012219897-35-5(R)-1-(amino(phenyl)methyl)naphthalen-2-ol
APER-0131616367-18-0(1R,3S)-3-(3-ethoxy-4-methoxyphenyl)-1-phenyl-2,3-dihydro-1H-naphtho[1,2-e][1,3]oxazine
APER-014199600-54-9lithium (methylsulfonyl)methanide
APER-0151616367-19-11-((R)-(((S)-1-(3-ethoxy-4-methoxyphenyl)-2-(methylsulfonyl)ethyl)amino)(phenyl)methyl)naphthalen-2-ol
APER-016608141-42-0(S)-1-(3-ethoxy-4-methoxyphenyl)-2-(methylsulfonyl)ethanamine
OptimisedRoute 4Steps 3 · Total yield /
Synthetic routes & intermediates Route 4
CodeCAS No.Intermediate
APER-0056296-53-3N-(1,3-dioxo-1,3-dihydroisobenzofuran-4-yl)acetamide
APER-00860758-86-33-ethoxy-4-methoxybenzonitrile
APER-016608141-42-0(S)-1-(3-ethoxy-4-methoxyphenyl)-2-(methylsulfonyl)ethanamine
APER-0171450657-31-4(E)-1-(3-ethoxy-4-methoxyphenyl)-2-(methylsulfonyl)ethenamine
OptimisedRoute 5Steps 7 · Total yield 49-54 g
Synthetic routes & intermediates Route 5
CodeCAS No.Intermediate
APER-0011131-52-83-ethoxy-4-methoxybenzaldehyde
APER-00860758-86-33-ethoxy-4-methoxybenzonitrile
APER-016608141-42-0(S)-1-(3-ethoxy-4-methoxyphenyl)-2-(methylsulfonyl)ethanamine
APER-0171450657-31-4(E)-1-(3-ethoxy-4-methoxyphenyl)-2-(methylsulfonyl)ethenamine
APER-0181450657-28-91-(3-ethoxy-4-methoxyphenyl)-2-(methylsulfonyl)ethanone
APER-0192627-86-3(S)-1-phenylethan-1-amine
APER-0201450759-47-31-(3-ethoxy-4-methoxyphenyl)-2-(methylsulfonyl)-N-((S)-1-phenylethyl)ethanamine hydrochloride
APER-021196929-78-9(R)-2-methylpropane-2-sulfinamide
APER-0221450759-43-9(E)-N-(3-ethoxy-4-methoxybenzylidene)-2-methylpropane-2-sulfinamide
APER-0231450759-44-0N-((S)-1-(3-ethoxy-4-methoxyphenyl)-2-(methylsulfonyl)ethyl)-2-methylpropane-2-sulfinamide
OptimisedRoute 6Steps 3 · Total yield 0.33 g
Synthetic routes & intermediates Route 6
CodeCAS No.Intermediate
APER-0031188-21-2(2S)-2-acetamido-4-methylpentanoic acid
APER-0181450657-28-91-(3-ethoxy-4-methoxyphenyl)-2-(methylsulfonyl)ethanone
APER-0241450657-24-5(R)-1-(3-ethoxy-4-methoxyphenyl)-2-(methylsulfonyl)ethanol
APER-0251450657-43-8(S)-4-(1-azido-2-(methylsulfonyl)ethyl)-2-ethoxy-1-methoxybenzene
APER-026608141-43-1(S)-1-(3-ethoxy-4-methoxyphenyl)-2-(methylsulfonyl)ethanamine (S)-2-acetamido-4-methylpentanoate

Frequently asked questions

What are the approved indications of Apremilast?

Approved indications include: Plaque psoriasis, Behçet's syndrome, Oral ulcer, Psoriasis, Psoriatic arthritis.

When does the Apremilast patent expire?

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

How many synthesis routes are recorded for Apremilast?

6 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 Apremilast intermediates?

All intermediates in Apremilast 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 Apremilast 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