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盐酸艾司氯胺酮
Tier B — Position earlyEsketamine Hydrochloride · all drugs expiring in 2029 →
辉瑞
Originator
1997
First approval
2029
Expiry (public)
$1.7B ▲
Peak sales
化学药
Type
Targets：NMDAR
Brand：Ketanest S、Spravato、Ketanest、Keyzilen、速开朗
Indications (approved)：重度抑郁症、自杀意念、抑郁症、麻醉、难治性抑郁症、疼痛
Regional status
US
批准上市
2019-03-05
EU
批准上市
1997-08-01
China
批准上市
2019-11-18
Japan
临床三期
2026-07-23
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 3 · Total yield 5.09 g (Esketamine Hydrochloride)
| Code | CAS No. | Intermediate |
|---|---|---|
| ESKE-001 | 6740-88-1 | 2-(2-chlorophenyl)-2-(methylamino)cyclohexan-1-one |
| ESKE-002 | 87-69-4 | (2R,3R)-2,3-dihydroxysuccinic acid |
| ESKE-003 | 199468-20-7 | (S)-2-(2-chlorophenyl)-2-(methylamino)cyclohexan-1-one (2R,3R)-2,3-dihydroxysuccinate |
| ESKE-004 | 33643-46-8 | (S)-2-(2-chlorophenyl)-2-(methylamino)cyclohexan-1-one |
OptimisedRoute 2Steps 4 · Total yield 6.60 mg (Esketamine Hydrochloride)
| Code | CAS No. | Intermediate |
|---|---|---|
| ESKE-005 | 615-41-8 | 1-chloro-2-iodobenzene |
| ESKE-006 | 108-94-1 | cyclohexanone |
| ESKE-007 | 91393-49-6 | 2-(2-chlorophenyl)cyclohexan-1-one |
| ESKE-008 | 870-50-8 | di-tert-butyl (E)-diazene-1,2-dicarboxylate |
| ESKE-009 | 1668563-29-8 | di-tert-butyl (S)-1-(1-(2-chlorophenyl)-2-oxocyclohexyl)hydrazine-1,2-dicarboxylate |
| ESKE-010 | 83777-65-5 | (S)-2-amino-2-(2-chlorophenyl)cyclohexan-1-one |
OptimisedRoute 3Steps 3 · Total yield /
| Code | CAS No. | Intermediate |
|---|---|---|
| (I)270899-1-a | 6740-85-8 | (2-Chlorophenyl)(cyclopentyl)methanone |
| (II)270899-1-a | 1823362-29-3 | 2-(2-Chlorophenyl)-2-hydroxycyclohexan-1-one |
| (III)270899-1-a | - | Aminomethane |
| (IV)270899-1-a | 6740-88-1 | 2-(2-Chlorophenyl)-2-(methylamino)cyclohexan-1-one |
| (V)270899-1-a | 33795-24-3 | (2R)-2-(2-Chlorophenyl)-2-(methylamino)cyclohexan-1-one hydrogen chloride |
| (VIa)270899-1-a | 33643-49-1 | (-)-2(R)-(2-Chlorophenyl)-2-(methylamino)cyclohexanone |
| (VIb)270899-1-a | - | Phosphoric acid (2R)-2-(2-chlorophenyl)-2-(methylamino)cyclohexan-1-one |
| (VIc)270899-1-a | - | Sulfuric acid (2R)-2-(2-chlorophenyl)-2-(methylamino)cyclohexan-1-one |
| (VId)270899-1-a | - | 2,3-Dihydroxybutanedioic acid (2R)-2-(2-chlorophenyl)-2-(methylamino)cyclohexan-1-one |
OptimisedRoute 4Steps 4 · Total yield /
| Code | CAS No. | Intermediate |
|---|---|---|
| (I)270899-2-a | 615-41-8 | 1-Chloro-2-iodobenzene |
| (II)270899-2-a | 108-94-1 | 4-Cyclohexanone |
| (III)270899-2-a | 91393-49-6 | 2-(2-Chlorophenyl)cyclohexanone |
| (IV)270899-2-a | - | (E)-Di-tert-butyl azodiformate |
| (V)270899-2-a | 1668563-29-8 | Di-tert-butyl 1-[(1S)-1-(2-chlorophenyl)-2-oxocyclohexyl]hydrazine-1,2-dicarboxylate |
| (VI)270899-2-a,(VI)270899-2-c | - | (-)-2(S)-Amino-2-(2-chlorophenyl)cyclohexanone |
| (VII)270899-2-a | 2375682-62-3 | (1S)-2'-Chloro-1-isocyanato-6-methoxy-1,2,3,4-tetrahydro-1,1'-biphenyl |
| (VIII)270899-2-a | 50-00-0Available | Formaldehyde |
| (IX)270899-2-a | 33643-46-8 | (2S)-2-(2-Chlorophenyl)-2-(methylamino)cyclohexanone |
OptimisedRoute 5Steps 2 · Total yield /
| Code | CAS No. | Intermediate |
|---|---|---|
| (X)270899-2-b | - | (aR)-3,3'-Diiodo-2,2'-bis(methoxymethoxy)-6,6'-dioctyl-1,1'-binaphthalene |
| (XI)270899-2-b | 820217-06-9 | Bromo(2,4,6-tricyclohexylphenyl)magnesium |
| (XII)270899-2-b | - | (aR)-6,6'-Dioctyl-3,3'-bis(2,4,6-tricyclohexylphenyl)-1,1'-binaphthalene-2,2'-diol |
OptimisedRoute 6Steps 2 · Total yield /
| Code | CAS No. | Intermediate |
|---|---|---|
| (VI)270899-2-a,(VI)270899-2-c | - | (-)-2(S)-Amino-2-(2-chlorophenyl)cyclohexanone |
| (XIII)270899-2-c | 1823362-29-3 | 2-(2-Chlorophenyl)-2-hydroxycyclohexan-1-one |
| (XIV)270899-2-c | 35211-10-0 | 2-Amino-2-(2-chlorophenyl)cyclohexanone |
| (XV)270899-2-c | 83777-68-8 | (2R)-2-Amino-2-(2-chlorophenyl)cyclohexan-1-one hydrogen chloride |
OptimisedRoute 7Steps 8 · Total yield /
| Code | CAS No. | Intermediate |
|---|---|---|
| (I)270899-3-a | 10316-66-2 | 2-Hydroxycyclohex-2-en-1-one |
| (II)270899-3-a | 10324-65-9 | 3-Bromo-2-hydroxycyclohex-2-en-1-one |
| (III)270899-3-a | 445249-11-6 | 3-Bromo-2-methoxycyclohex-2-en-1-one |
| (IV)270899-3-a | 23740-37-6 | 2-Methoxycyclohex-2-en-1-one |
| (V)270899-3-a | 3900-89-8 | (o-Chlorophenyl)boronic acid |
| (VI)270899-3-a | 2375682-55-4 | 2'-Chloro-2-methoxy-5,6-dihydro[1,1'-biphenyl]-3(4H)-one |
| (VII)270899-3-a | 2375682-66-7 | (3S)-2'-Chloro-2-methoxy-3,4,5,6-tetrahydro[1,1'-biphenyl]-3-ol |
| (VIII)270899-3-a | 3019-71-4 | 2,2,2-Trichloro-N-(oxomethylidene)acetamide |
| (IX)270899-3-a | 2375682-61-2 | (3S)-2'-Chloro-2-methoxy-3,4,5,6-tetrahydro[1,1'-biphenyl]-3-yl carbamate |
| (X)270899-3-a | 2375682-62-3 | (1S)-2'-Chloro-1-isocyanato-6-methoxy-1,2,3,4-tetrahydro-1,1'-biphenyl |
| (XI)270899-3-a | 2375682-63-4 | (1S)-2'-Chloro-6-methoxy-N-methyl-3,4-dihydro[1,1'-biphenyl]-1(2H)-amine |
OptimisedRoute 8Steps 6 · Total yield /
| Code | CAS No. | Intermediate |
|---|---|---|
| (I)270899-4-a | 74-88-4Available | Iodomethane |
| (II)270899-4-a | 930-28-9Available | Chlorocyclopentane |
| (III)270899-4-a | 873-32-5 | 1-Chloro-2-cyanobenzene |
| (IV)270899-4-a | 6740-85-8 | (2-Chlorophenyl)(cyclopentyl)methanone |
| (V)270899-4-a | 609-65-4 | 2-Chlorobenzoyl chloride |
| (VI)270899-4-a | 142-29-0 | Cyclopentene |
| (VII)270899-4-a | 6740-86-9 | (1-Bromocyclopentyl)(2-chlorophenyl) ketone |
| (VIII)270899-4-a | - | Aminomethane |
| (IX)270899-4-a | - | 1-[(E)-(2-Chlorophenyl)(methylimino)methyl]cyclopentan-1-ol hydrogen chloride |
| (Xa)270899-4-a | 1867-66-9 | (±)-2-(2-Chlorophenyl)-2-(methylamino)cyclohexanone hydrochloride |
| (Xb)270899-4-a | 6740-88-1 | 2-(2-Chlorophenyl)-2-(methylamino)cyclohexan-1-one |
| (XI)270899-4-a | 33643-46-8 | (2S)-2-(2-Chlorophenyl)-2-(methylamino)cyclohexanone |
Frequently asked questions
What are the approved indications of Esketamine Hydrochloride?
Approved indications include: 重度抑郁症, 自杀意念, 抑郁症, 麻醉, 难治性抑郁症, 疼痛.
When does the Esketamine Hydrochloride patent expire?
Based on public sources, the Esketamine Hydrochloride patent expires in 2029.
How many synthesis routes are recorded for Esketamine Hydrochloride?
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 Esketamine Hydrochloride intermediates?
3 intermediate CAS of Esketamine Hydrochloride 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 Esketamine Hydrochloride 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