← Back to patent-cliff list
Mufemilast
Tier C — Watch / tradeMufemilast
-
Originator
2025
First approval
-
Expiry (public)
No sales data
Peak sales
Small molecule
Type
Targets：IL1R, TNFα, PDE4B, PDE4
Indications (approved)：Plaque psoriasis
Regional status
US
-
EU
-
China
Approved
2025-09-30
Japan
-
Synthetic routes & intermediates4 routes
Originator routes × 0Optimised (non-patent) × 4Process 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.
OptimisedRoute 1Steps 8 · Total yield /
(I)989842-1-a3141-26-2(II)989842-1-a18853-32-2(III)989842-1-a4282-29-5(IV)989842-1-a6007-85-8(V)989842-1-a932032-15-0(VI)989842-1-a932032-16-1(VII)989842-1-a,(VII)989842-1-b608141-42-0(VIII)989842-1-a1255908-99-6(IX)989842-1-a—(Xa)989842-1-a108-24-7(Xb)989842-1-a75-36-5API · Mufemilast
| Code | CAS No. | Intermediate |
|---|---|---|
| (I)989842-1-a | 3141-26-2 | 3,4-Bis(bromanyl)thiophene |
| (II)989842-1-a | 18853-32-2 | 3,4-Dicyanothiophene |
| (III)989842-1-a | 4282-29-5 | Thiophene-3,4-dicarboxylic acid |
| (IV)989842-1-a | 6007-85-8 | 1H,3H-Thieno[3,4-c]furan-1,3-dione |
| (V)989842-1-a | 932032-15-0 | 2-Nitrothiophene-3,4-dicarboxylic acid |
| (VI)989842-1-a | 932032-16-1 | 4-Nitro-1H,3H-thieno[3,4-c]furan-1,3-dione |
| (VII)989842-1-a,(VII)989842-1-b | 608141-42-0 | (1S)-1-(3-Ethoxy-4-methoxyphenyl)-2-(methylsulfonyl)ethanamine |
| (VIII)989842-1-a | 1255908-99-6 | 3-Nitro-5-[1(S)-(3-ethoxy-4-methoxyphenyl)-2-methylsulfonylethyl]thieno[3,4-c]pyrrole-4,6-dione |
| (IX)989842-1-a | - | 1-Amino-5-[(1S)-1-(3-ethoxy-4-methoxyphenyl)-2-(methanesulfonyl)ethyl]-4H-thieno[3,4-c]pyrrole-4,6(5H)-dione |
| (Xa)989842-1-a | 108-24-7 | Acetic acid acetic anhydride |
| (Xb)989842-1-a | 75-36-5 | Acetic acid chloride |
OptimisedRoute 2Steps 4 · Total yield /
(VII)989842-1-a,(VII)989842-1-b608141-42-0(XI)989842-1-b621-59-0(XII)989842-1-b75-03-6(XIII)989842-1-b1131-52-8(XIV)989842-1-b4039-32-1(XV)989842-1-b67-71-0(XVI)989842-1-b—(XVII)989842-1-b253168-94-4API · Mufemilast
| Code | CAS No. | Intermediate |
|---|---|---|
| (VII)989842-1-a,(VII)989842-1-b | 608141-42-0 | (1S)-1-(3-Ethoxy-4-methoxyphenyl)-2-(methylsulfonyl)ethanamine |
| (XI)989842-1-b | 621-59-0 | 3-Hydroxy-4-methoxybenzaldehyde |
| (XII)989842-1-b | 75-03-6Available | 1-Iodoethane |
| (XIII)989842-1-b | 1131-52-8 | (3-Ethoxy-4-methoxy-phenyl)-methanone |
| (XIV)989842-1-b | 4039-32-1 | 1,1,1-Trimethyl-N-(trimethylsilyl)silanamine lithium salt |
| (XV)989842-1-b | 67-71-0 | 1-(Methylsulfonyl)methane |
| (XVI)989842-1-b | - | 1-(3-Ethoxy-4-methoxyphenyl)-2-methylsulfonyl-N-trimethylsilylethanamine |
| (XVII)989842-1-b | 253168-94-4 | 1-(3-Ethoxy-4-methoxyphenyl)-2-(methylsulfonyl)ethanamine |
OptimisedRoute 3Steps 5 · Total yield /
(Ia)989842-2-a—(Ib)989842-2-a—(II)989842-2-a1510155-99-3(III)989842-2-a,(III)989842-2-b608141-42-0(IV)989842-2-a—(Va)989842-2-a108-24-7(Vb)989842-2-a75-36-5(VI)989842-2-a—(VII)989842-2-a—API · Mufemilast
| Code | CAS No. | Intermediate |
|---|---|---|
| (Ia)989842-2-a | - | 3-tert-Butyl 4-methyl 2-aminothiophene-3,4-dicarboxylate |
| (Ib)989842-2-a | - | 3-Benzyl 4-methyl 2-aminothiophene-3,4-dicarboxylate |
| (II)989842-2-a | 1510155-99-3 | 2-Amino-4-(methoxycarbonyl)thiophene-3-carboxylic acid |
| (III)989842-2-a,(III)989842-2-b | 608141-42-0 | (1S)-1-(3-Ethoxy-4-methoxyphenyl)-2-(methylsulfonyl)ethanamine |
| (IV)989842-2-a | - | Methyl 5-amino-4-[[(1S)-1-(3-ethoxy-4-methoxyphenyl)-2-(methanesulfonyl)ethyl]carbamoyl]thiophene-3-carboxylate |
| (Va)989842-2-a | 108-24-7 | Acetic acid acetic anhydride |
| (Vb)989842-2-a | 75-36-5 | Acetic acid chloride |
| (VI)989842-2-a | - | Methyl 5-acetamido-4-[[(1S)-1-(3-ethoxy-4-methoxyphenyl)-2-(methanesulfonyl)ethyl]carbamoyl]thiophene-3-carboxylate |
| (VII)989842-2-a | - | 5-Acetamido-4-[[(1S)-1-(3-ethoxy-4-methoxyphenyl)-2-(methanesulfonyl)ethyl]carbamoyl]thiophene-3-carboxylic acid |
OptimisedRoute 4Steps 5 · Total yield /
(III)989842-2-a,(III)989842-2-b608141-42-0(VIII)989842-2-b60758-86-3(IX)989842-2-b67-71-0(X)989842-2-b1715011-38-3(XI)989842-2-b1450657-28-9(XII)989842-2-b2627-86-3(XIII)989842-2-b1800584-69-3(XIV)989842-2-b1450759-41-7(XV)989842-2-b1131-52-8(XVI)989842-2-b196929-78-9(XVII)989842-2-b—(XVIII)989842-2-b1450759-44-0API · Mufemilast
| Code | CAS No. | Intermediate |
|---|---|---|
| (III)989842-2-a,(III)989842-2-b | 608141-42-0 | (1S)-1-(3-Ethoxy-4-methoxyphenyl)-2-(methylsulfonyl)ethanamine |
| (VIII)989842-2-b | 60758-86-3 | 3-Ethoxy-4-methoxybenzonitrile |
| (IX)989842-2-b | 67-71-0 | 1-(Methylsulfonyl)methane |
| (X)989842-2-b | 1715011-38-3 | 1-(3-Ethoxy-4-methoxyphenyl)-2-(mesyl)ethenamine |
| (XI)989842-2-b | 1450657-28-9 | 1-(3-Ethoxy-4-methoxyphenyl)-2-(methanesulfonyl)ethan-1-one |
| (XII)989842-2-b | 2627-86-3 | (S)-(-)-1-Phenylethylamine |
| (XIII)989842-2-b | 1800584-69-3 | 1-(3-Ethoxy-4-methoxyphenyl)-2-(methylsulfonyl)-N-[(1S)-1-phenylethyl]ethenamine |
| (XIV)989842-2-b | 1450759-41-7 | (1S)-1-(3-Ethoxy-4-methoxyphenyl)-2-(methanesulfonyl)-N-[(1S)-1-phenylethyl]ethan-1-amine |
| (XV)989842-2-b | 1131-52-8 | (3-Ethoxy-4-methoxy-phenyl)-methanone |
| (XVI)989842-2-b | 196929-78-9 | (+)-(R)-2-Methylpropane-2-sulfinamide |
| (XVII)989842-2-b | - | (SR)-N-[(3-Ethoxy-4-methoxyphenyl)methyl]-2-methylpropane-2-sulfinamide |
| (XVIII)989842-2-b | 1450759-44-0 | N-[(1S)-1-(3-Ethoxy-4-methoxyphenyl)-2-(methylsulfonyl)ethyl]-2-methylpropane-2-sulfinamide |
Frequently asked questions
What are the approved indications of Mufemilast?
Approved indications include: Plaque psoriasis.
When does the Mufemilast patent expire?
No public expiry year is available for Mufemilast yet; this page updates once verified.
How many synthesis routes are recorded for Mufemilast?
4 synthesis routes are recorded; the shortest is 4 steps with / total yield. Intermediates in each route carry codes and CAS numbers.
Where can I buy Mufemilast intermediates?
1 intermediate CAS of Mufemilast 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 Mufemilast 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) · 2026-10-22