阿普米司特
Tier B — Position earlyApremilast · all drugs expiring in 2028 →
Targets：PDE4
Brand：欧泰乐、Otezla
Indications (approved)：斑块银屑病、白塞病综合征、口腔溃疡、银屑病、银屑病关节炎
Regional status
Synthetic routes & intermediates6 routes
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.
| Code | CAS No. | Intermediate |
|---|---|---|
| APER-001 | 1131-52-8 | 3-ethoxy-4-methoxybenzaldehyde |
| APER-002 | 253168-94-4 | 1-(3-ethoxy-4-methoxyphenyl)-2-(methylsulfonyl)ethan-1-amine |
| APER-003 | 1188-21-2 | (2S)-2-acetamido-4-methylpentanoic acid |
| APER-004 | 608141-43-1 | (S)-1-(3-ethoxy-4-methoxyphenyl)-2-(methylsulfonyl)ethanamine (S)-2-acetamido-4-methylpentanoate |
| APER-005 | 6296-53-3 | N-(1,3-dioxo-1,3-dihydroisobenzofuran-4-yl)acetamide |
| APER-006 | 603-11-2 | 3-nitrophthalic acid |
| APER-007 | 5434-20-8 | 3-aminophthalic acid |
| Code | CAS No. | Intermediate |
|---|---|---|
| APER-001 | 1131-52-8 | 3-ethoxy-4-methoxybenzaldehyde |
| APER-002 | 253168-94-4 | 1-(3-ethoxy-4-methoxyphenyl)-2-(methylsulfonyl)ethan-1-amine |
| APER-006 | 603-11-2 | 3-nitrophthalic acid |
| APER-008 | 60758-86-3 | 3-ethoxy-4-methoxybenzonitrile |
| APER-009 | 641-70-3 | 4-nitroisobenzofuran-1,3-dione |
| APER-010 | 253168-82-0 | 2-(1-(3-ethoxy-4-methoxyphenyl)-2-(methylsulfonyl)ethyl)-4-nitroisoindoline-1,3-dione |
| APER-011 | 253168-83-1 | 4-amino-2-(1-(3-ethoxy-4-methoxyphenyl)-2-(methylsulfonyl)ethyl)isoindoline-1,3-dione |
| Code | CAS No. | Intermediate |
|---|---|---|
| APER-001 | 1131-52-8 | 3-ethoxy-4-methoxybenzaldehyde |
| APER-005 | 6296-53-3 | N-(1,3-dioxo-1,3-dihydroisobenzofuran-4-yl)acetamide |
| APER-012 | 219897-35-5 | (R)-1-(amino(phenyl)methyl)naphthalen-2-ol |
| APER-013 | 1616367-18-0 | (1R,3S)-3-(3-ethoxy-4-methoxyphenyl)-1-phenyl-2,3-dihydro-1H-naphtho[1,2-e][1,3]oxazine |
| APER-014 | 199600-54-9 | lithium (methylsulfonyl)methanide |
| APER-015 | 1616367-19-1 | 1-((R)-(((S)-1-(3-ethoxy-4-methoxyphenyl)-2-(methylsulfonyl)ethyl)amino)(phenyl)methyl)naphthalen-2-ol |
| APER-016 | 608141-42-0 | (S)-1-(3-ethoxy-4-methoxyphenyl)-2-(methylsulfonyl)ethanamine |
| Code | CAS No. | Intermediate |
|---|---|---|
| APER-005 | 6296-53-3 | N-(1,3-dioxo-1,3-dihydroisobenzofuran-4-yl)acetamide |
| APER-008 | 60758-86-3 | 3-ethoxy-4-methoxybenzonitrile |
| APER-016 | 608141-42-0 | (S)-1-(3-ethoxy-4-methoxyphenyl)-2-(methylsulfonyl)ethanamine |
| APER-017 | 1450657-31-4 | (E)-1-(3-ethoxy-4-methoxyphenyl)-2-(methylsulfonyl)ethenamine |
| Code | CAS No. | Intermediate |
|---|---|---|
| APER-001 | 1131-52-8 | 3-ethoxy-4-methoxybenzaldehyde |
| APER-008 | 60758-86-3 | 3-ethoxy-4-methoxybenzonitrile |
| APER-016 | 608141-42-0 | (S)-1-(3-ethoxy-4-methoxyphenyl)-2-(methylsulfonyl)ethanamine |
| APER-017 | 1450657-31-4 | (E)-1-(3-ethoxy-4-methoxyphenyl)-2-(methylsulfonyl)ethenamine |
| APER-018 | 1450657-28-9 | 1-(3-ethoxy-4-methoxyphenyl)-2-(methylsulfonyl)ethanone |
| APER-019 | 2627-86-3 | (S)-1-phenylethan-1-amine |
| APER-020 | 1450759-47-3 | 1-(3-ethoxy-4-methoxyphenyl)-2-(methylsulfonyl)-N-((S)-1-phenylethyl)ethanamine hydrochloride |
| APER-021 | 196929-78-9 | (R)-2-methylpropane-2-sulfinamide |
| APER-022 | 1450759-43-9 | (E)-N-(3-ethoxy-4-methoxybenzylidene)-2-methylpropane-2-sulfinamide |
| APER-023 | 1450759-44-0 | N-((S)-1-(3-ethoxy-4-methoxyphenyl)-2-(methylsulfonyl)ethyl)-2-methylpropane-2-sulfinamide |
| Code | CAS No. | Intermediate |
|---|---|---|
| APER-003 | 1188-21-2 | (2S)-2-acetamido-4-methylpentanoic acid |
| APER-018 | 1450657-28-9 | 1-(3-ethoxy-4-methoxyphenyl)-2-(methylsulfonyl)ethanone |
| APER-024 | 1450657-24-5 | (R)-1-(3-ethoxy-4-methoxyphenyl)-2-(methylsulfonyl)ethanol |
| APER-025 | 1450657-43-8 | (S)-4-(1-azido-2-(methylsulfonyl)ethyl)-2-ethoxy-1-methoxybenzene |
| APER-026 | 608141-43-1 | (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: 斑块银屑病, 白塞病综合征, 口腔溃疡, 银屑病, 银屑病关节炎.
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) · 2026-09-24