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Elinzanetant
Tier C — Watch / tradeElinzanetant
GSK
Originator
2025
First approval
-
Expiry (public)
No sales data
Peak sales
Small molecule
Type
Targets：NK1R, NK3R
Brand：Lynkuet
Indications (approved)：Hot flushes, Vasomotor symptoms
Regional status
US
Approved
2025-10-24
EU
Approved
2025-07-10
China
Phase I
2022-05-23
Japan
Phase I
2021-08-11
Synthetic routes & intermediates5 routes
Originator routes × 0Optimised (non-patent) × 5Process 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 10 · Total yield 280 mg (Elinzanetant)
Elinzanetant-001212650-43-6Elinzanetant-002955401-37-3Elinzanetant-003929047-52-9Elinzanetant-004929047-53-0Elinzanetant-005929047-30-3Elinzanetant-006825643-73-0Elinzanetant-007929047-32-5Elinzanetant-0082135332-08-8Elinzanetant-0091256823-62-7Elinzanetant-010139911-29-8Elinzanetant-011825643-62-7Elinzanetant-012289686-69-7API · Elinzanetant
| Code | CAS No. | Intermediate |
|---|---|---|
| Elinzanetant-001 | 212650-43-6Available | 4-(tert-butoxycarbonyl)morpholine-3-carboxylic acid |
| Elinzanetant-002 | 955401-37-3Available | tert-butyl 3-(((R)-3-hydroxy-1-methoxy-1-oxopropan-2-yl)carbamoyl)morpholine-4-carboxylate |
| Elinzanetant-003 | 929047-52-9Available | (7R)-7-(hydroxymethyl)hexahydropyrazino[2,1-c][1,4]oxazine-6,9-dione |
| Elinzanetant-004 | 929047-53-0Available | ((7S)-octahydropyrazino[2,1-c][1,4]oxazin-7-yl)methanol |
| Elinzanetant-005 | 929047-30-3Available | (7S,9aS)-7-(((tert-butyldimethylsilyl)oxy)methyl)octahydropyrazino[2,1-c][1,4]oxazine |
| Elinzanetant-006 | 825643-73-0Available | 2-(3,5-bis(trifluoromethyl)phenyl)-N-(6-chloro-4-(4-fluoro-2-methylphenyl)pyridin-3-yl)-N,2-dimethylpropanamide |
| Elinzanetant-007 | 929047-32-5Available | 2-(3,5-bis(trifluoromethyl)phenyl)-N-(6-((7S,9aS)-7-(((tert-butyldimethylsilyl)oxy)methyl)hexahydropyrazino[2,1-c][1,4]oxazin-8(1H)-yl)-4-(4-fluoro-2-methylphenyl)pyridin-3-yl)-N,2-dimethylpropanamide |
| Elinzanetant-008 | 2135332-08-8Available | tert-butyl (6-chloro-4-methylpyridin-3-yl)(methyl)carbamate |
| Elinzanetant-009 | 1256823-62-7Available | 6-chloro-N,4-dimethylpyridin-3-amine |
| Elinzanetant-010 | 139911-29-8Available | (4-fluoro-2-methylphenyl)boronic acid |
| Elinzanetant-011 | 825643-62-7Available | 6-chloro-4-(4-fluoro-2-methylphenyl)-N-methylpyridin-3-amine |
| Elinzanetant-012 | 289686-69-7Available | 2-(3,5-bis(trifluoromethyl)phenyl)-2-methylpropanoyl chloride |
OptimisedRoute 2Steps 8 · Total yield /
(I)448314-1-a5350-93-6(II)448314-1-a171178-45-3(III)448314-1-a400777-00-6(IV)448314-1-a74-88-4(V)448314-1-a825643-58-1(VI)448314-1-a825643-59-2(VII)448314-1-a139911-29-8(VIII)448314-1-a825643-62-7(IX)448314-1-a289686-69-7(X)448314-1-a—(XI)448314-1-a,(XI)448314-1-b929047-30-3(XII)448314-1-a—API · Elinzanetant
| Code | CAS No. | Intermediate |
|---|---|---|
| (I)448314-1-a | 5350-93-6Available | 3-Amino-6-chloropyridine |
| (II)448314-1-a | 171178-45-3Available | 1,1-Dimethylethyl (6-Chloro-3-pyridinyl)carbamate |
| (III)448314-1-a | 400777-00-6Available | N-(6-Chloro-4-iodopyridin-3-yl)carbamic acid tert-butyl ester |
| (IV)448314-1-a | 74-88-4Available | Iodomethane |
| (V)448314-1-a | 825643-58-1Available | 6-Chloro-4-iodo-N-methyl-N-Boc-pyridin-3-amine |
| (VI)448314-1-a | 825643-59-2Available | 6-Chloro-4-iodo-N-methylpyridin-3-amine |
| (VII)448314-1-a | 139911-29-8Available | 4-Fluoro-2-methylphenylboronic acid |
| (VIII)448314-1-a | 825643-62-7Available | 6-Chloro-4-(4-fluoro-2-methylphenyl)-N-methylpyridin-3-amine |
| (IX)448314-1-a | 289686-69-7Available | 2-[3,5-Bis(trifluoromethyl)phenyl]-2-methylpropanoyl chloride |
| (X)448314-1-a | - | 2-[3,5-Bis(trifluoromethyl)phenyl]-N-[6-chloro-4-(4-fluoro-2-methylphenyl)pyridin-3-yl]-N,2-dimethylpropanamide |
| (XI)448314-1-a,(XI)448314-1-b | 929047-30-3Available | (7S,9aS)-7-([[tert-Butyl(dimethyl)silyl]oxy]methyl)octahydropyrazino[2,1-c][1,4]oxazine |
| (XII)448314-1-a | - | 2-[3,5-Bis(trifluoromethyl)phenyl]-N-[6-[(7S,9aS)-7-([[tert-butyl(dimethyl)silyl]oxy]methyl)hexahydropyrazino[2,1-c][1,4]oxazin-8(1H)-yl]-4-(4-fluoro-2-methylphenyl)pyridin-3-yl]-N,2-dimethylpropanamide |
OptimisedRoute 3Steps 6 · Total yield /
(XI)448314-1-a,(XI)448314-1-b929047-30-3(XIII)448314-1-b212650-43-6(XIV)448314-1-b5874-57-7(XIX)448314-1-b869681-70-9(XV)448314-1-b—(XVI)448314-1-b929047-27-8(XVII)448314-1-b929047-29-0(XVIII)448314-1-b131110-76-4(XX)448314-1-b—(XXI)448314-1-b—(XXII)448314-1-b—(XXIII)448314-1-b—API · Elinzanetant
| Code | CAS No. | Intermediate |
|---|---|---|
| (XI)448314-1-a,(XI)448314-1-b | 929047-30-3Available | (7S,9aS)-7-([[tert-Butyl(dimethyl)silyl]oxy]methyl)octahydropyrazino[2,1-c][1,4]oxazine |
| (XIII)448314-1-b | 212650-43-6Available | 4-[(tert-Butoxy)carbonyl]morpholine-3-carboxylic acid |
| (XIV)448314-1-b | 5874-57-7Available | (R)-Methyl 2-amino-3-hydroxypropanoate hydrochloride |
| (XIX)448314-1-b | 869681-70-9Available | (3R)-4-(tert-Butoxycarbonyl)morpholine-3-carboxylic acid |
| (XV)448314-1-b | - | tert-Butyl 3-[[(2R)-3-hydroxy-1-methoxy-1-oxopropan-2-yl]carbamoyl]morpholine-4-carboxylate |
| (XVI)448314-1-b | 929047-27-8Available | (7R)-7-(Hydroxymethyl)hexahydropyrazino[2,1-c][1,4]oxazine-6,9-dione |
| (XVII)448314-1-b | 929047-29-0Available | [(7S)-Octahydropyrazino[2,1-c][1,4]oxazin-7-yl]methanol |
| (XVIII)448314-1-b | 131110-76-4Available | N-Benzyl-D-serine methyl ester |
| (XX)448314-1-b | - | tert-Butyl (3R)-3-[benzyl[(2R)-3-hydroxy-1-methoxy-1-oxopropan-2-yl]carbamoyl]morpholine-4-carboxylate |
| (XXI)448314-1-b | - | (7R,9aR)-8-Benzyl-7-(hydroxymethyl)hexahydropyrazino[2,1-c][1,4]oxazine-6,9-dione |
| (XXII)448314-1-b | - | [(7S,9aS)-8-Benzyloctahydropyrazino[2,1-c][1,4]oxazin-7-yl]methanol |
| (XXIII)448314-1-b | - | (7S,9aS)-8-Benzyl-7-([[tert-butyl(dimethyl)silyl]oxy]methyl)octahydropyrazino[2,1-c][1,4]oxazine |
OptimisedRoute 4Steps 10 · Total yield /
(I)448314-2-a106910-77-4(II)448314-2-a79-04-9(III)448314-2-a106973-36-8(IV)448314-2-a—(V)448314-2-a218594-79-7(VI)448314-2-a47173-80-8(VII)448314-2-a—(VIII)448314-2-a—(IX)448314-2-a—(X)448314-2-a—(XI)448314-2-a—(XII)448314-2-a,(XII)448314-2-b—(XIIIa)448314-2-a—(XIIIb)448314-2-a—API · Elinzanetant
| Code | CAS No. | Intermediate |
|---|---|---|
| (I)448314-2-a | 106910-77-4Available | N-Benzyl-D-serine |
| (II)448314-2-a | 79-04-9Available | 2-Chloranylethanoyl chloride |
| (III)448314-2-a | 106973-36-8Available | 4-Benzyl-5-oxomorpholine-3(R)-carboxylic acid |
| (IV)448314-2-a | - | [(3S)-4-Benzylmorpholin-3-yl]methanol hydrogen chloride (1/1) |
| (V)448314-2-a | 218594-79-7Available | [(3S)-Morpholin-3-yl]methanol hydrogen chloride (1/1) |
| (VI)448314-2-a | 47173-80-8Available | 3-(Benzyloxy)-2(R)-(tert-butoxycarbonylamino)propionic acid |
| (VII)448314-2-a | - | tert-Butyl [(2R)-3-(benzyloxy)-1-[(3S)-3-(hydroxymethyl)morpholin-4-yl]-1-oxopropan-2-yl]carbamate |
| (VIII)448314-2-a | - | tert-Butyl [(2S)-1-(benzyloxy)-3-[(3S)-3-(hydroxymethyl)morpholin-4-yl]propan-2-yl]carbamate |
| (IX)448314-2-a | - | tert-Butyl [(2S)-1-(benzyloxy)-3-[(3R)-3-(chloromethyl)morpholin-4-yl]propan-2-yl]carbamate |
| (X)448314-2-a | - | (2S)-1-(Benzyloxy)-3-[(3R)-3-(chloromethyl)morpholin-4-yl]propan-2-amine |
| (XI)448314-2-a | - | (7S,9aS)-7-[(Benzyloxy)methyl]octahydropyrazino[2,1-c][1,4]oxazine |
| (XII)448314-2-a,(XII)448314-2-b | - | 2-[3,5-Bis(trifluoromethyl)phenyl]-N-[6-chloro-4-(4-fluoro-2-methylphenyl)pyridin-3-yl]-N,2-dimethylpropanamide |
| (XIIIa)448314-2-a | - | N-[6-[(7S,9aS)-7-[(Benzyloxy)methyl]hexahydropyrazino[2,1-c][1,4]oxazin-8(1H)-yl]-4-(4-fluoro-2-methylphenyl)pyridin-3-yl]-2-[3,5-bis(trifluoromethyl)phenyl]-N,2-dimethylpropanamide hydrogen chloride (1/2) |
| (XIIIb)448314-2-a | - | N-[6-[(7S,9aS)-7-[(Benzyloxy)methyl]hexahydropyrazino[2,1-c][1,4]oxazin-8(1H)-yl]-4-(4-fluoro-2-methylphenyl)pyridin-3-yl]-2-[3,5-bis(trifluoromethyl)phenyl]-N,2-dimethylpropanamide |
OptimisedRoute 5Steps 5 · Total yield /
(XII)448314-2-a,(XII)448314-2-b—(XIV)448314-2-b850663-54-6(XIX)448314-2-b289686-69-7(XV)448314-2-b139911-29-8(XVI)448314-2-b2642577-27-1(XVII)448314-2-b2642577-29-3(XVIII)448314-2-b—(XX)448314-2-b289686-70-0(XXI)448314-2-b—(XXII)448314-2-b74-88-4API · Elinzanetant
| Code | CAS No. | Intermediate |
|---|---|---|
| (XII)448314-2-a,(XII)448314-2-b | - | 2-[3,5-Bis(trifluoromethyl)phenyl]-N-[6-chloro-4-(4-fluoro-2-methylphenyl)pyridin-3-yl]-N,2-dimethylpropanamide |
| (XIV)448314-2-b | 850663-54-6Available | 4-Chloro-5-nitropyridin-2(1H)-one |
| (XIX)448314-2-b | 289686-69-7Available | 2-[3,5-Bis(trifluoromethyl)phenyl]-2-methylpropanoyl chloride |
| (XV)448314-2-b | 139911-29-8Available | 4-Fluoro-2-methylphenylboronic acid |
| (XVI)448314-2-b | 2642577-27-1Available | 4-(4-Fluoro-2-methylphenyl)-5-nitropyridin-2(1H)-one |
| (XVII)448314-2-b | 2642577-29-3Available | 2-Chloro-4-(4-fluoro-2-methylphenyl)-5-nitropyridine |
| (XVIII)448314-2-b | - | 6-Chloro-4-(4-fluoro-2-methylphenyl)pyridin-3-amine hydrogen chloride (1/1) |
| (XX)448314-2-b | 289686-70-0Available | 2-[3,5-Bis(trifluoromethyl)phenyl]-2-methylpropanoic acid |
| (XXI)448314-2-b | - | 2-[3,5-Bis(trifluoromethyl)phenyl]-N-[6-chloro-4-(4-fluoro-2-methylphenyl)pyridin-3-yl]-2-methylpropanamide |
| (XXII)448314-2-b | 74-88-4Available | Iodomethane |
Frequently asked questions
What are the approved indications of Elinzanetant?
Approved indications include: Hot flushes, Vasomotor symptoms.
When does the Elinzanetant patent expire?
No public expiry year is available for Elinzanetant yet; this page updates once verified.
How many synthesis routes are recorded for Elinzanetant?
5 synthesis routes are recorded; the shortest is 5 steps with / total yield. Intermediates in each route carry codes and CAS numbers.
Where can I buy Elinzanetant intermediates?
32 intermediate CAS of Elinzanetant 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 Elinzanetant 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