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Norketotifen
Tier C — Watch / tradeNorketotifen
Emergo Therapeutics Inc
Originator
-
First approval
-
Expiry (public)
No sales data
Peak sales
Small molecule
Type
Targets：HRH1
Indications (approved)：Influenza virus infection, Allergic conjunctivitis, Allergic rhinitis
Regional status
US
Phase II
2019-04-01
EU
-
China
-
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 1 · Total yield 14.74 g (Norketotifen)
Ketotifen34580-13-7Norketotifen34580-20-6API · Norketotifen
| Code | CAS No. | Intermediate |
|---|---|---|
| Ketotifen | 34580-13-7 | 4-(1-methylpiperidin-4-ylidene)-4H-benzo[4,5]cyclohepta[1,2-b]thiophen-10(9H)-one |
| Norketotifen | 34580-20-6 | 4-(piperidin-4-ylidene)-4H-benzo[4,5]cyclohepta[1,2-b]thiophen-10(9H)-one |
OptimisedRoute 2Steps 7 · Total yield /
(I)471701-1-a4506-53-0(II)471701-1-a,(II)471701-1-b34580-10-4(III)471701-1-a43076-89-7(IV)471701-1-a59743-84-9(V)471701-1-a,(V)471701-1-b63463-36-5(VI)471701-1-a5570-77-4(VII)471701-1-a59743-88-3(VIII)471701-1-a,(VIII)471701-1-b34580-13-7(IXa)471701-1-a34580-19-3(IXb)471701-1-a—API · Norketotifen
| Code | CAS No. | Intermediate |
|---|---|---|
| (I)471701-1-a | 4506-53-0 | 6-Thiatricyclo[8.4.0.0(3,7)]tetradeca-1(14),3(7),4,8,10,12-hexaen-2-one |
| (II)471701-1-a,(II)471701-1-b | 34580-10-4 | 8,9-Dibromo-6-thiatricyclo[8.4.0.0(3,7)]tetradeca-1(10),3(7),4,11,13-pentaen-2-one |
| (III)471701-1-a | 43076-89-7 | 9-Bromo-10-methoxy-9,10-dihydro-4H-benzo[4,5]cyclohepta[1,2-b]thiophen-4-one |
| (IV)471701-1-a | 59743-84-9Available | 10-Methoxy-4H-benzo[4,5]cyclohepta[1,2-b]thiophen-4-one |
| (V)471701-1-a,(V)471701-1-b | 63463-36-5 | 1-Methylpiperidn-4-ylmagnesium chloride |
| (VI)471701-1-a | 5570-77-4 | 4-Chloro-1-methylpiperidine |
| (VII)471701-1-a | 59743-88-3 | 10-Methoxy-4-(1-methylpiperidin-4-yl)-4H-benzo[4,5]cyclohepta[1,2-b]thiophene-4-ol |
| (VIII)471701-1-a,(VIII)471701-1-b | 34580-13-7 | 4-(1-Methyl-4-piperidinylidene)-4,9-dihydro-10H-benzo[4,5]cyclohepta[1,2-b]thiophen-10-one |
| (IXa)471701-1-a | 34580-19-3 | 4-[8-Oxo-6-thiatricyclo[8.4.0.0(3,7)]tetradeca-1(14),3(7),4,10,12-pentaen-2-ylidene]piperidine-1-carboxylic acid ethyl ester |
| (IXb)471701-1-a | - | 1-Chloroethyl 4-(10-oxo-9,10-dihydro-4H-benzo[4,5]cyclohepta[1,2-b]thiophen-4-ylidene)piperidine-1-carboxylate |
OptimisedRoute 3Steps 6 · Total yield /
(II)471701-1-a,(II)471701-1-b34580-10-4(V)471701-1-a,(V)471701-1-b63463-36-5(VIII)471701-1-a,(VIII)471701-1-b34580-13-7(X)471701-1-b1622-55-5(XI)471701-1-b34580-11-5(XII)471701-1-b59776-37-3(XIII)471701-1-b34580-12-6(XIV)471701-1-b110-89-4(XV)471701-1-b59743-85-0(XVI)471701-1-b59743-86-1(XVII)471701-1-b34580-09-1API · Norketotifen
| Code | CAS No. | Intermediate |
|---|---|---|
| (II)471701-1-a,(II)471701-1-b | 34580-10-4 | 8,9-Dibromo-6-thiatricyclo[8.4.0.0(3,7)]tetradeca-1(10),3(7),4,11,13-pentaen-2-one |
| (V)471701-1-a,(V)471701-1-b | 63463-36-5 | 1-Methylpiperidn-4-ylmagnesium chloride |
| (VIII)471701-1-a,(VIII)471701-1-b | 34580-13-7 | 4-(1-Methyl-4-piperidinylidene)-4,9-dihydro-10H-benzo[4,5]cyclohepta[1,2-b]thiophen-10-one |
| (X)471701-1-b | 1622-55-5Available | 6-thiatricyclo[8.4.0.0(3,7)]tetradeca-1(10),3(7),4,11,13-pentaen-2-one |
| (XI)471701-1-b | 34580-11-5 | 8-bromo-6-thiatricyclo[8.4.0.0(3,7)]tetradeca-1(10),3(7),4,8,11,13-hexaen-2-one |
| (XII)471701-1-b | 59776-37-3 | 8-bromo-2-(1-methylpiperidin-4-yl)-6-thiatricyclo[8.4.0.0(3,7)]tetradeca-1(10),3(7),4,8,11,13-hexaen-2-ol |
| (XIII)471701-1-b | 34580-12-6 | 4-{8-bromo-6-thiatricyclo[8.4.0.0(3,7)]tetradeca-1(10),3(7),4,8,11,13-hexaen-2-ylidene}-1-methylpiperidine |
| (XIV)471701-1-b | 110-89-4 | Azacyclohexane |
| (XV)471701-1-b | 59743-85-0 | 1-Methyl-4-[9-(piperidin-1-yl)-6-thiatricyclo[8.4.0.0(3,7)]tetradeca-1(14),3(7),4,8,10,12-hexaen-2-ylidene]piperidine |
| (XVI)471701-1-b | 59743-86-1 | 1-methyl-4-[8-(piperidin-1-yl)-6-thiatricyclo[8.4.0.0(3,7)]tetradeca-1(10),3(7),4,8,11,13-hexaen-2-ylidene]piperidine |
| (XVII)471701-1-b | 34580-09-1 | 2-(1-Methylpiperidin-4-ylidene)-6-thiatricyclo[8.4.0.0(3,7)]tetradeca-1(14),3(7),4,10,12-pentaen-9-one |
OptimisedRoute 4Steps 2 · Total yield /
(I)471701-2-a34580-13-7(IIa)471701-2-a108-24-7(IIb)471701-2-a1609-47-8(IIc)471701-2-a123-62-6(IId)471701-2-a93-97-0(IIe)471701-2-a31139-36-3(IIf)471701-2-a106-31-0(IIIa)471701-2-a117540-07-5(IIIb)471701-2-a34580-19-3(IIIc)471701-2-a2489527-25-3(IIId)471701-2-a2489527-27-5(IIIe)471701-2-a2489527-28-6(IIIf)471701-2-a2489527-26-4API · Norketotifen
| Code | CAS No. | Intermediate |
|---|---|---|
| (I)471701-2-a | 34580-13-7 | 4-(1-Methyl-4-piperidinylidene)-4,9-dihydro-10H-benzo[4,5]cyclohepta[1,2-b]thiophen-10-one |
| (IIa)471701-2-a | 108-24-7 | Acetic acid acetic anhydride |
| (IIb)471701-2-a | 1609-47-8 | Dicarbonic acid diethyl diester |
| (IIc)471701-2-a | 123-62-6Available | Methylacetic anhydride |
| (IId)471701-2-a | 93-97-0 | Benzoic acid anhydride |
| (IIe)471701-2-a | 31139-36-3 | Dibenzyl dicarbonate |
| (IIf)471701-2-a | 106-31-0 | Butanoic acid 1-oxobutyl ester |
| (IIIa)471701-2-a | 117540-07-5 | 4-(1-Acetylpiperidin-4-ylidene)-4,9-dihydro-10H-benzo[4,5]cyclohepta[1,2-b]thiophen-10-one |
| (IIIb)471701-2-a | 34580-19-3 | 4-[8-Oxo-6-thiatricyclo[8.4.0.0(3,7)]tetradeca-1(14),3(7),4,10,12-pentaen-2-ylidene]piperidine-1-carboxylic acid ethyl ester |
| (IIIc)471701-2-a | 2489527-25-3 | 4-(1-Propanoylpiperidin-4-ylidene)-4,9-dihydro-10H-benzo[4,5]cyclohepta[1,2-b]thiophen-10-one |
| (IIId)471701-2-a | 2489527-27-5 | 4-(1-Benzoylpiperidin-4-ylidene)-4,9-dihydro-10H-benzo[4,5]cyclohepta[1,2-b]thiophen-10-one |
| (IIIe)471701-2-a | 2489527-28-6 | Benzyl 4-(10-oxo-9,10-dihydro-4H-benzo[4,5]cyclohepta[1,2-b]thiophen-4-ylidene)piperidine-1-carboxylate |
| (IIIf)471701-2-a | 2489527-26-4 | 4-(1-Butanoylpiperidin-4-ylidene)-4,9-dihydro-10H-benzo[4,5]cyclohepta[1,2-b]thiophen-10-one |
Frequently asked questions
What are the approved indications of Norketotifen?
Approved indications include: Influenza virus infection, Allergic conjunctivitis, Allergic rhinitis.
When does the Norketotifen patent expire?
No public expiry year is available for Norketotifen yet; this page updates once verified.
How many synthesis routes are recorded for Norketotifen?
4 synthesis routes are recorded; the shortest is 1 steps with 14.74 g (Norketotifen) total yield. Intermediates in each route carry codes and CAS numbers.
Where can I buy Norketotifen intermediates?
3 intermediate CAS of Norketotifen 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 Norketotifen 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) · 2026-10-08