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氯苯唑酸
Tier C — Watch / tradeTafamidis
辉瑞
Originator
2019
First approval
-
Expiry (public)
No sales data
Peak sales
化学药
Type
Targets：TTR
Brand：维万心、VYNDAMAX
Indications (approved)：转甲状腺素运载蛋白淀粉样变性、心脏病
Regional status
US
批准上市
2019-05-03
EU
临床一期
2024-02-27
China
批准上市
2020-09-30
Japan
临床一期
2026-05-11
Synthetic routes & intermediates8 routes
Originator routes × 0Optimised (non-patent) × 8Process 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 5 · Total yield /
| Code | CAS No. | Intermediate |
|---|---|---|
| (I)409139-2-a | 2374-03-0 | (4-Carboxy-2-hydroxyphenyl)amine |
| (II)409139-2-a | 149-73-5 | Orthoformic acid trimethyl ester |
| (III)409139-2-a | - | 1,3-Benzoxazole-6-carboxylic acid |
| (IV)409139-2-a | - | 1,3-Benzoxazole-6-carbonyl chloride |
| (V)409139-2-a | 1334429-35-4 | 1,3-Benzoxazol-6-yl(morpholin-4-yl)methanone |
| (VI)409139-2-a | 3032-81-3 | 1,3-Dichloro-5-iodobenzene |
| (VII)409139-2-a | - | [2-(3,5-Dichlorophenyl)-1,3-benzoxazol-6-yl]-morpholinomethanone |
| (VIII)409139-2-a | 594839-88-0 | 2-(3,5-Dichlorophenyl)benzo[d]oxazole-6-carboxylic acid |
OptimisedRoute 2Steps 4 · Total yield /
| Code | CAS No. | Intermediate |
|---|---|---|
| (I)409139-3-a | 2905-62-6 | 3,5-Dichloro-1-benzenecarbonyl chloride |
| (II)409139-3-a | 1624066-48-3 | 3,5-Dichloro-N-methyl-N-phenylbenzamide |
| (III)409139-3-a | 2650595-66-5 | N-[(3,5-Dichlorophenyl)(methoxy)methylidene]-N-methylbenzeniminium trifluoromethanesulfonate |
| (IV)409139-3-a | 1692797-15-1 | 1,3-Dichloro-5-(trimethoxymethyl)benzene |
| (V)409139-3-a | 4704-99-8 | 2-(Hydroxymethyl)-2-phenylpropane-1,3-diol |
| (VI)409139-3-a | 122-78-1 | 2-Phenylacetaldehyde |
| (VII)409139-3-a | 77-99-6 | 2-Ethyl-2-(hydroxymethyl)propane-1,3-diol |
| (VIIIa)409139-3-a | 2650595-70-1 | 1-(3,5-Dichlorophenyl)-4-phenyl-2,6,7-trioxabicyclo[2.2.2]octane |
| (VIIIb)409139-3-a | 2650595-69-8 | 1-(3,5-Dichlorophenyl)-4-ethyl-2,6,7-trioxabicyclo[2.2.2]octane |
| (IX)409139-3-a | 2374-03-0 | (4-Carboxy-2-hydroxyphenyl)amine |
| (X)409139-3-a | 594839-88-0 | 2-(3,5-Dichlorophenyl)benzo[d]oxazole-6-carboxylic acid |
OptimisedRoute 3Steps 3 · Total yield /
| Code | CAS No. | Intermediate |
|---|---|---|
| (I)409139-4-a | 2905-62-6 | 3,5-Dichloro-1-benzenecarbonyl chloride |
| (II)409139-4-a | 3143-02-0 | (3-Methyloxetan-3-yl)methanol |
| (III)409139-4-a | 2650595-67-6 | (3-Methyloxetan-3-yl)methyl 3,5-dichlorobenzoate |
| (IV)409139-4-a | 2650595-68-7 | 1-(3,5-Dichlorophenyl)-4-methyl-2,6,7-trioxabicyclo[2.2.2]octane |
| (V)409139-4-a | 2374-03-0 | (4-Carboxy-2-hydroxyphenyl)amine |
| (VI)409139-4-a | 594839-88-0 | 2-(3,5-Dichlorophenyl)benzo[d]oxazole-6-carboxylic acid |
OptimisedRoute 4Steps 3 · Total yield /
| Code | CAS No. | Intermediate |
|---|---|---|
| (Ia)409139-5-a | 590-86-3 | 3-Methylbutanal |
| (Ib)409139-5-a | 2987-16-8 | 3,3-Dimethylbutanal |
| (IIa)409139-5-a | 20762-78-1 | 2-(Hydroxymethyl)-2-(propan-2-yl)propane-1,3-diol |
| (IIb)409139-5-a | 67590-29-8 | 2-tert-Butyl-2-(hydroxymethyl)propane-1,3-diol |
| (III)409139-5-a | 51-36-5 | 3,5-Dichlorobenzoic acid |
| (IVa)409139-5-a | 2650595-75-6 | 1-(3,5-Dichlorophenyl)-4-(propan-2-yl)-2,6,7-trioxabicyclo[2.2.2]octane |
| (IVb)409139-5-a | 2650595-77-8 | 4-tert-Butyl-1-(3,5-dichlorophenyl)-2,6,7-trioxabicyclo[2.2.2]octane |
| (V)409139-5-a | 2374-03-0 | (4-Carboxy-2-hydroxyphenyl)amine |
| (VI)409139-5-a | 594839-88-0 | 2-(3,5-Dichlorophenyl)benzo[d]oxazole-6-carboxylic acid |
OptimisedRoute 5Steps 2 · Total yield /
| Code | CAS No. | Intermediate |
|---|---|---|
| (I)409139-6-a | 1692797-15-1 | 1,3-Dichloro-5-(trimethoxymethyl)benzene |
| (II)409139-6-a | 3068-00-6 | (±)-1,2,4-Butanetriol |
| (III)409139-6-a | 2650595-73-4 | 1-(3,5-Dichlorophenyl)-2,7,8-trioxabicyclo[3.2.1]octane |
| (IV)409139-6-a | 107-21-1Available | 1,2-Dihydroxyethane |
| (V)409139-6-a | 2650595-72-3 | 2-(3,5-Dichlorophenyl)-2-methoxy-1,3-dioxolane |
| (VI)409139-6-a | 2041-15-8 | cis-Cyclohexane-1,3,5-triol |
| (VII)409139-6-a | 2650595-74-5 | 3-(3,5-Dichlorophenyl)-2,4,10-trioxaadamantane |
| (VIII)409139-6-a | 2374-03-0 | (4-Carboxy-2-hydroxyphenyl)amine |
| (IX)409139-6-a | 594839-88-0 | 2-(3,5-Dichlorophenyl)benzo[d]oxazole-6-carboxylic acid |
OptimisedRoute 6Steps 2 · Total yield /
| Code | CAS No. | Intermediate |
|---|---|---|
| (Ia)409139-7-a | 10203-08-4Available | 3,5-Dichlorobenzaldehyde |
| (Ib)409139-7-a | 51-36-5 | 3,5-Dichlorobenzoic acid |
| (IIa)409139-7-a | 2835-98-5 | 2-Amino-5-methylphenol |
| (IIb)409139-7-a | 182499-90-7 | 1-Amino-2-hydroxy-4-ethylbenzene |
| (IIc)409139-7-a | 2316835-58-0 | 2-Amino-5-butylphenol |
| (IId)409139-7-a | 2374-03-0 | (4-Carboxy-2-hydroxyphenyl)amine |
| (IIIa)409139-7-a | 1414840-15-5 | 2-(3,5-Dichlorophenyl)-6-methyl-1,3-benzoxazole |
| (IIIb)409139-7-a | 2761347-26-4 | 2-(3,5-Dichlorophenyl)-6-ethyl-1,3-benzoxazole |
| (IIIc)409139-7-a | 2761347-28-6 | 6-Butyl-2-(3,5-dichlorophenyl)-1,3-benzoxazole |
| (IV)409139-7-a | 594839-88-0 | 2-(3,5-Dichlorophenyl)benzo[d]oxazole-6-carboxylic acid |
| (V)409139-7-a | - | 4-([(1E)-(3,5-Dichlorophenyl)methylene]amino)-3-hydroxybenzoic acid |
OptimisedRoute 7Steps 2 · Total yield /
| Code | CAS No. | Intermediate |
|---|---|---|
| (I)409139-9-a | - | 1-Ethyl-3-hydroxybenzene |
| (II)409139-9-a | 39989-43-0 | (3,5-Dichlorophenyl)methanamine |
| (III)409139-9-a | 2761347-26-4 | 2-(3,5-Dichlorophenyl)-6-ethyl-1,3-benzoxazole |
| (IV)409139-9-a | 594839-88-0 | 2-(3,5-Dichlorophenyl)benzo[d]oxazole-6-carboxylic acid |
| (V)409139-9-a | 17159-79-4 | 4-Oxocyclohexanecarboxylic acid ethyl ester |
| (VI)409139-9-a | - | Ethyl 2-(3,5-dichlorophenyl)-1,3-benzoxazole-6-carboxylate |
OptimisedRoute 8Steps 4 · Total yield /
| Code | CAS No. | Intermediate |
|---|---|---|
| (I)409139-12-a | 626-43-7 | 3,5-Dichloroaniline |
| (II)409139-12-a | 431-03-8 | 2,3-Butanedione |
| (III)409139-12-a | 14401-72-0 | 1-(3,5-Dichlorophenyl)ethanone |
| (IV)409139-12-a | - | (3,5-Dichlorophenyl)(oxo)acetic acid |
| (V)409139-12-a | 2835-98-5 | 2-Amino-5-methylphenol |
| (VI)409139-12-a | 1414840-15-5 | 2-(3,5-Dichlorophenyl)-6-methyl-1,3-benzoxazole |
| (VII)409139-12-a | 594839-88-0 | 2-(3,5-Dichlorophenyl)benzo[d]oxazole-6-carboxylic acid |
Frequently asked questions
What are the approved indications of Tafamidis?
Approved indications include: 转甲状腺素运载蛋白淀粉样变性, 心脏病.
When does the Tafamidis patent expire?
No public expiry year is available for Tafamidis yet; this page updates once verified.
How many synthesis routes are recorded for Tafamidis?
8 synthesis routes are recorded; the shortest is 2 steps with / total yield. Intermediates in each route carry codes and CAS numbers.
Where can I buy Tafamidis intermediates?
2 intermediate CAS of Tafamidis 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 Tafamidis 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