Ketoconazole

Tier C — Watch / trade

Ketoconazole

Johnson & Johnson

Originator

1981

First approval

Expiry (public)

No sales data

Peak sales

Small molecule

Type

Targets：CYP51A1

Brand：Xolegel, Nizoral, Extina, Kuric, Panfungol, Ketoderm, <span class="highlightText">Ketoconazole</span> HRA, Sebazole

Indications (approved)：Cushing's syndrome, 头皮屑, Pityriasis versicolor, 皮肤念珠菌病, Tinea, 脂溢性皮炎, Candidiasis, 足癣

Regional status

Approved

1981-06-12

Approved

2014-11-18

China

Approved

1990-01-01

Japan

Approved

1993-12-01

Synthetic routes & intermediates4 routes

Originator routes × 0Optimised (non-patent) × 3Process routes × 1

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 2Steps 4 · Total yield 21.26g(Ketoconazole FREE)

Ketoconazole-013541-73-1Ketoconazole-01413094-51-4Ketoconazole-015598-21-0Ketoconazole-0012631-72-3Ketoconazole-016288-32-4,1467-16-9Ketoconazole-01746503-52-0Ketoconazole-01067914-60-7Ketoconazole-018106-89-8Ketoconazole-019—API · Ketoconazole

Code	CAS No.	Intermediate
Ketoconazole-013	541-73-1	1,3-Dichlorobenzene
Ketoconazole-014	13094-51-4 Available	2-Bromoacetyl 2-bromoacetate
Ketoconazole-015	598-21-0	2-Bromoacetyl bromide
Ketoconazole-001	2631-72-3	2-Bromo-1-(2,4-dichlorophenyl)ethanone
Ketoconazole-016	288-32-4,1467-16-9	1,3-Diaza-2,4-cyclopentadiene
Ketoconazole-017	46503-52-0	1-(2,4-Dichlorophenyl)-2-imidazolylethanone
Ketoconazole-010	67914-60-7	1-[4-(4-Hydroxyphenyl)piperazin-1-yl]ethanone
Ketoconazole-018	106-89-8	(+/-)-2-(Chloromethyl)oxirane
Ketoconazole-019	-	1-[4-[4-(2,3-Dihydroxypropoxy)phenyl]piperazin-1-yl]ethan-1-one

OptimisedRoute 3Steps 5 · Total yield 295g(Ketoconazole-023)

Ketoconazole-013541-73-1Ketoconazole-02079-04-9Ketoconazole-0214252-78-2Ketoconazole-016288-32-4,1467-16-9Ketoconazole-01746503-52-0Ketoconazole-00356-81-5Ketoconazole-02284682-23-5Ketoconazole-008134071-44-6Ketoconazole-0231610851-14-3API · Ketoconazole

Code	CAS No.	Intermediate
Ketoconazole-013	541-73-1	1,3-Dichlorobenzene
Ketoconazole-020	79-04-9 Available	2-Chloroacetyl chloride
Ketoconazole-021	4252-78-2	omega,2,4-Trichloroacetophenone
Ketoconazole-016	288-32-4,1467-16-9	1,3-Diaza-2,4-cyclopentadiene
Ketoconazole-017	46503-52-0	1-(2,4-Dichlorophenyl)-2-imidazolylethanone
Ketoconazole-003	56-81-5	Glycerol
Ketoconazole-022	84682-23-5	(±)-[2-(2,4-Dichlorophenyl)-2-[(1H-imidazol-1-yl)methyl]-1,3-dioxolan-4-yl]methanol
Ketoconazole-008	134071-44-6	[cis-2-(2,4-Dichlorophenyl)-2-[(1H-imidazol-1-yl)methyl]-1,3-dioxolan-4-yl]methanol
Ketoconazole-023	1610851-14-3	[(2S,4S)-2-(2,4-Dichlorophenyl)-2-[(1H-imidazol-1-yl)methyl]-1,3-dioxolan-4-yl]methyl 4-methylbenzene-1-sulfonate

OptimisedRoute 4Steps 1 · Total yield /

Ketoconazole-024106-37-6Ketoconazole-025100-79-8Ketoconazole-026198275-89-7API · Ketoconazole

Code	CAS No.	Intermediate
Ketoconazole-024	106-37-6 Available	1,4-Dibromobenzene
Ketoconazole-025	100-79-8	(2,2-Dimethyl-1,3-dioxolan-4-yl)methanol
Ketoconazole-026	198275-89-7	4-[(4-Bromophenoxy)methyl]-2,2-dimethyl-1,3-dioxolane

ProcessRoute 1Steps 7 · Total yield 338g(Ketoconazole FREE)

Ketoconazole-0012631-72-3Ketoconazole-0022234-16-4Ketoconazole-00356-81-5Ketoconazole-004512791-61-6Ketoconazole-005170210-46-5Ketoconazole-0061467-16-9,288-32-4Ketoconazole-007—Ketoconazole-008134071-44-6Ketoconazole-009170210-50-1Ketoconazole-01067914-60-7Ketoconazole-01156621-48-8Ketoconazole-012108-24-7API · Ketoconazole

Code	CAS No.	Intermediate
Ketoconazole-001	2631-72-3	2-Bromo-2',4'-dichloroacetophenone
Ketoconazole-002	2234-16-4	2',4'-Dichloroacetophenone
Ketoconazole-003	56-81-5	Glycerol
Ketoconazole-004	512791-61-6	[(2S,4R)-2-(bromomethyl)-2-(2,4-dichlorophenyl)-1,3-dioxolan-4-yl]methanol
Ketoconazole-005	170210-46-5	(±)-cis-2-(Bromomethyl)-2-(2,4-dichlorophenyl)-1,3-dioxolan-4-yl]methyl benzoate
Ketoconazole-006	1467-16-9,288-32-4	Imidazole
Ketoconazole-007	-	[(2S,4S)-2-(2,4-dichlorophenyl)-2-(1H-imidazol-1-ylmethyl)-1,3-dioxolan-4-yl]methyl benzoate
Ketoconazole-008	134071-44-6	[cis-2-(2,4-Dichlorophenyl)-2-[(1H-imidazol-1-yl)methyl]-1,3-dioxolan-4-yl]methanol
Ketoconazole-009	170210-50-1	[(2S,4S)-2-(2,4-Dichlorophenyl)-2-(1H-imidazol-1-ylmethyl)-1,3-dioxolan-4-yl]methyl methanesulfonate
Ketoconazole-010	67914-60-7	1-[4-(4-Hydroxyphenyl)piperazin-1-yl]ethanone
Ketoconazole-011	56621-48-8	4-(Piperazin-1-yl)phenol
Ketoconazole-012	108-24-7	Acetic anhydride

Frequently asked questions

What are the approved indications of Ketoconazole?

Approved indications include: Cushing's syndrome, 头皮屑, Pityriasis versicolor, 皮肤念珠菌病, Tinea, 脂溢性皮炎, Candidiasis, 足癣.

When does the Ketoconazole patent expire?

No public expiry year is available for Ketoconazole yet; this page updates once verified.

How many synthesis routes are recorded for Ketoconazole?

4 synthesis routes are recorded; the shortest is 1 steps with / total yield. Intermediates in each route carry codes and CAS numbers.

Where can I buy Ketoconazole intermediates?

3 intermediate CAS of Ketoconazole 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 Ketoconazole 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) · 2026-09-27