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Lotilaner
Tier C — Watch / tradeLotilaner
Elanco Tiergesundheit Ag
Originator
2023
First approval
-
Expiry (public)
No sales data
Peak sales
Small molecule
Type
Targets：mites GABA-gated chloride channel
Brand：XDEMVY
Indications (approved)：蠕形螨性睑缘炎
Regional status
US
Approved
2023-07-24
EU
-
China
Approved
2026-03-17
Japan
-
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 8 · Total yield /
(I)700647-1-a14282-78-1(II)700647-1-a1862972-98-2(III)700647-1-a75-16-1(IV)700647-1-a13679-73-7(IX)700647-1-a—(V)700647-1-a,(V)700647-1-d859199-06-7(VI)700647-1-a,(VI)700647-1-d158401-00-4(VII)700647-1-a,(VII)700647-1-d—(VIII)700647-1-a,(VIII)700647-1-d5470-11-1(X)700647-1-a—(XI)700647-1-a,(XI)700647-1-d—(XII)700647-1-a,(XII)700647-1-b1171331-39-7(XIII)700647-1-a,(XIII)700647-1-c21928-51-8(XIV)700647-1-a—(XV)700647-1-a1547-87-1API · Lotilaner
| Code | CAS No. | Intermediate |
|---|---|---|
| (I)700647-1-a | 14282-78-1Available | 4-Methylthiophene-2-carboxylic acid |
| (II)700647-1-a | 1862972-98-2Available | N-Methoxy-N,4-dimethylthiophene-2-carboxamide |
| (III)700647-1-a | 75-16-1Available | Bromo(methyl)magnesium |
| (IV)700647-1-a | 13679-73-7Available | 1-(4-Methylthiophen-2-yl)ethan-1-one |
| (IX)700647-1-a | - | 3-(5-Bromo-4-methylthiophen-2-yl)-5-(3,4,5-trichlorophenyl)-5-(trifluoromethyl)-4,5-dihydro-1,2-oxazole |
| (V)700647-1-a,(V)700647-1-d | 859199-06-7Available | 1-(5-Bromo-4-methylthiophen-2-yl)ethan-1-one |
| (VI)700647-1-a,(VI)700647-1-d | 158401-00-4Available | 2,2,2-Trifluoro-1-(3,4,5-trichlorophenyl)ethan-1-one |
| (VII)700647-1-a,(VII)700647-1-d | - | 1-(5-Bromo-4-methylthiophen-2-yl)-4,4,4-trifluoro-3-(3,4,5-trichlorophenyl)but-2-en-1-one |
| (VIII)700647-1-a,(VIII)700647-1-d | 5470-11-1Available | Amino alcohol hydrochloride |
| (X)700647-1-a | - | 3-Methyl-5-[5-(3,4,5-trichlorophenyl)-5-(trifluoromethyl)-4,5-dihydro-1,2-oxazol-3-yl]thiophene-2-carboxylic acid |
| (XI)700647-1-a,(XI)700647-1-d | - | 3-Methyl-5-[(5S)-5-(3,4,5-trichlorophenyl)-5-(trifluoromethyl)-4,5-dihydro-1,2-oxazol-3-yl]thiophene-2-carboxylic acid |
| (XII)700647-1-a,(XII)700647-1-b | 1171331-39-7Available | 2-Amino-N-(2,2,2-trifluoroethyl)acetamide hydrochloride |
| (XIII)700647-1-a,(XIII)700647-1-c | 21928-51-8Available | 5-Bromo-1,2,3-trichlorobenzene |
| (XIV)700647-1-a | - | (3,4,5-Trichlorophenyl)magnesium bromide |
| (XV)700647-1-a | 1547-87-1Available | 2,2,2-Trifluoro-N,N-dimethylacetamide |
OptimisedRoute 2Steps 3 · Total yield /
(XII)700647-1-a,(XII)700647-1-b1171331-39-7(XIX)700647-1-b142955-50-8(XVIa)700647-1-b1138-80-3(XVIb)700647-1-b4530-20-5(XVIIa)700647-1-b373-88-6(XVIIb)700647-1-b753-90-2(XVIIIa)700647-1-b1371632-79-9(XVIIIb)700647-1-b1231755-15-9(XX)700647-1-b79-04-9(XXI)700647-1-b170655-44-4(XXII)700647-1-b103-49-1(XXIII)700647-1-b—API · Lotilaner
| Code | CAS No. | Intermediate |
|---|---|---|
| (XII)700647-1-a,(XII)700647-1-b | 1171331-39-7Available | 2-Amino-N-(2,2,2-trifluoroethyl)acetamide hydrochloride |
| (XIX)700647-1-b | 142955-50-8Available | 2,5-Dioxo-3-oxazolidinecarboxylic acid 1,1-dimethylethyl ester |
| (XVIa)700647-1-b | 1138-80-3Available | 2-(Benzyloxycarbonylamino)acetic acid |
| (XVIb)700647-1-b | 4530-20-5Available | 2-((tert-Butoxycarbonyl)amino)acetic acid |
| (XVIIa)700647-1-b | 373-88-6Available | 2-Amino-1,1,1-trifluoroethane hydrochloride |
| (XVIIb)700647-1-b | 753-90-2Available | 2-Amino-1,1,1-trifluoroethane |
| (XVIIIa)700647-1-b | 1371632-79-9Available | Benzyl [2-oxo-2-[(2,2,2-trifluoroethyl)amino]ethyl]carbamate |
| (XVIIIb)700647-1-b | 1231755-15-9Available | [(2,2,2-Trifluoroethylcarbamoyl)methyl]carbamic acid tert-butyl ester |
| (XX)700647-1-b | 79-04-9Available | 2-Chloranylethanoyl chloride |
| (XXI)700647-1-b | 170655-44-4Available | 2-Chloro-N-(2,2,2-trifluoroethyl)acetamide |
| (XXII)700647-1-b | 103-49-1Available | (N-Benzylaminomethyl)benzene |
| (XXIII)700647-1-b | - | 2-(Dibenzylamino)-N-(2,2,2-trifluoroethyl)acetamide |
OptimisedRoute 3Steps 3 · Total yield /
(XIII)700647-1-a,(XIII)700647-1-c21928-51-8(XXIV)700647-1-c63-74-1(XXV)700647-1-c22134-75-4(XXVI)700647-1-c697-88-1(XXVII)700647-1-c62-53-3(XXVIII)700647-1-c106-40-1API · Lotilaner
| Code | CAS No. | Intermediate |
|---|---|---|
| (XIII)700647-1-a,(XIII)700647-1-c | 21928-51-8Available | 5-Bromo-1,2,3-trichlorobenzene |
| (XXIV)700647-1-c | 63-74-1Available | 4-(Aminosulfonyl)aniline |
| (XXV)700647-1-c | 22134-75-4Available | 3,5-Dichlorosulfanilamide |
| (XXVI)700647-1-c | 697-88-1Available | (4-Bromo-2,6-dichlorophenyl)amine |
| (XXVII)700647-1-c | 62-53-3Available | Aminobenzene |
| (XXVIII)700647-1-c | 106-40-1Available | p-Bromoaniline |
OptimisedRoute 4Steps 7 · Total yield /
(V)700647-1-a,(V)700647-1-d859199-06-7(VI)700647-1-a,(VI)700647-1-d158401-00-4(VII)700647-1-a,(VII)700647-1-d—(VIII)700647-1-a,(VIII)700647-1-d5470-11-1(XI)700647-1-a,(XI)700647-1-d—(XXIX)700647-1-d—(XXX)700647-1-d—(XXXI)700647-1-d—(XXXII)700647-1-d,(XXXII)700647-1-e2758907-87-6(XXXIII)700647-1-d—(XXXIV)700647-1-d7803-49-8(XXXV)700647-1-d—(XXXVI)700647-1-d—API · Lotilaner
| Code | CAS No. | Intermediate |
|---|---|---|
| (V)700647-1-a,(V)700647-1-d | 859199-06-7Available | 1-(5-Bromo-4-methylthiophen-2-yl)ethan-1-one |
| (VI)700647-1-a,(VI)700647-1-d | 158401-00-4Available | 2,2,2-Trifluoro-1-(3,4,5-trichlorophenyl)ethan-1-one |
| (VII)700647-1-a,(VII)700647-1-d | - | 1-(5-Bromo-4-methylthiophen-2-yl)-4,4,4-trifluoro-3-(3,4,5-trichlorophenyl)but-2-en-1-one |
| (VIII)700647-1-a,(VIII)700647-1-d | 5470-11-1Available | Amino alcohol hydrochloride |
| (XI)700647-1-a,(XI)700647-1-d | - | 3-Methyl-5-[(5S)-5-(3,4,5-trichlorophenyl)-5-(trifluoromethyl)-4,5-dihydro-1,2-oxazol-3-yl]thiophene-2-carboxylic acid |
| (XXIX)700647-1-d | - | 2-(5-Bromo-4-methylthiophen-2-yl)-2-methyl-1,3-dioxolane |
| (XXX)700647-1-d | - | 3-Methyl-5-(2-methyl-1,3-dioxolan-2-yl)thiophene-2-carboxylic acid |
| (XXXI)700647-1-d | - | Methyl 3-methyl-5-(2-methyl-1,3-dioxolan-2-yl)thiophene-2-carboxylate |
| (XXXII)700647-1-d,(XXXII)700647-1-e | 2758907-87-6Available | Methyl 5-acetyl-3-methylthiophene-2-carboxylate |
| (XXXIII)700647-1-d | - | Methyl 3-methyl-5-[4,4,4-trifluoro-3-(3,4,5-trichlorophenyl)but-2-enoyl]thiophene-2-carboxylate |
| (XXXIV)700647-1-d | 7803-49-8Available | Amine N-oxide |
| (XXXV)700647-1-d | - | Methyl 3-methyl-5-[(5S)-5-(3,4,5-trichlorophenyl)-5-(trifluoromethyl)-4,5-dihydro-1,2-oxazol-3-yl]thiophene-2-carboxylate |
| (XXXVI)700647-1-d | - | (5S)-3-(5-Bromo-4-methylthiophen-2-yl)-5-(3,4,5-trichlorophenyl)-5-(trifluoromethyl)-4,5-dihydro-1,2-oxazole |
OptimisedRoute 5Steps 2 · Total yield /
(XXXII)700647-1-d,(XXXII)700647-1-e2758907-87-6(XXXIX)700647-1-e2758907-91-2(XXXVII)700647-1-e23806-24-8(XXXVIII)700647-1-e78191-00-1API · Lotilaner
| Code | CAS No. | Intermediate |
|---|---|---|
| (XXXII)700647-1-d,(XXXII)700647-1-e | 2758907-87-6Available | Methyl 5-acetyl-3-methylthiophene-2-carboxylate |
| (XXXIX)700647-1-e | 2758907-91-2Available | 5-Acetyl-3-methylthiophene-2-carboxylic acid |
| (XXXVII)700647-1-e | 23806-24-8Available | 2-Carboxy-3-methylthiophene |
| (XXXVIII)700647-1-e | 78191-00-1Available | N-Acetyl-N,O-dimethylhydroxylamine |
OptimisedRoute 6Steps 5 · Total yield /
(I)700647-2-a1368183-08-7(II)700647-2-a5470-11-1(III)700647-2-a2382920-59-2(IV)700647-2-a359821-38-8(V)700647-2-a—(VI)700647-2-a—(VII)700647-2-a—(VIII)700647-2-a—(IX)700647-2-a864736-87-8(X)700647-2-a—API · Lotilaner
| Code | CAS No. | Intermediate |
|---|---|---|
| (I)700647-2-a | 1368183-08-7Available | 5-Formyl-3-methylthiophene-2-carboxylic acid |
| (II)700647-2-a | 5470-11-1Available | Amino alcohol hydrochloride |
| (III)700647-2-a | 2382920-59-2Available | 5-[(Hydroxyimino)methyl]-3-methylthiophene-2-carboxylic acid |
| (IV)700647-2-a | 359821-38-8Available | 2-Amino-N-(2,2,2-trifluoroethyl)acetamide |
| (V)700647-2-a | - | 5-[(Hydroxyimino)methyl]-3-methyl-N-[2-oxo-2-[(2,2,2-trifluoroethyl)amino]ethyl]thiophene-2-carboxamide |
| (VI)700647-2-a | - | 5-Formyl-3-methyl-N-[2-oxo-2-[(2,2,2-trifluoroethyl)amino]ethyl]thiophene-2-carboxamide |
| (VII)700647-2-a | - | N-Hydroxy-4-methyl-5-([2-oxo-2-[(2,2,2-trifluoroethyl)amino]ethyl]carbamoyl)thiophene-2-carboximidoyl chloride |
| (VIII)700647-2-a | - | 4-Methyl-5-([2-oxo-2-[(2,2,2-trifluoroethyl)amino]ethyl]carbamoyl)thiophene-2-carbonitrile oxide |
| (IX)700647-2-a | 864736-87-8Available | 1,2,3-Trichloro-5-(3,3,3-trifluoroprop-1-en-2-yl)benzene |
| (X)700647-2-a | - | (±)-3-Methyl-N-[2-oxo-2-[(2,2,2-trifluoroethyl)amino]ethyl]-5-[5-(3,4,5-trichlorophenyl)-5-(trifluoromethyl)-4,5-dihydro-1,2-oxazol-3-yl]thiophene-2-carboxamide |
OptimisedRoute 7Steps 6 · Total yield /
(I)700647-3-a5834-16-2(II)700647-3-a38239-46-2(III)700647-3-a38239-45-1(IV)700647-3-a75-52-5(V)700647-3-a2624121-17-9(VI)700647-3-a—(VII)700647-3-a864736-87-8(VIII)700647-3-a—(IX)700647-3-a1171331-39-7API · Lotilaner
| Code | CAS No. | Intermediate |
|---|---|---|
| (I)700647-3-a | 5834-16-2Available | 2-Formyl-3-methylthiophene |
| (II)700647-3-a | 38239-46-2Available | 5-Bromo-3-methylthiophene-2-carbaldehyde |
| (III)700647-3-a | 38239-45-1Available | 5-Bromo-3-methylthiophene-2-carboxylic acid |
| (IV)700647-3-a | 75-52-5Available | Nitrocarbol |
| (V)700647-3-a | 2624121-17-9Available | 3-Methyl-5-(nitromethyl)thiophene-2-carboxylic acid |
| (VI)700647-3-a | - | 5-Carboxy-4-methylthiophene-2-carbonitrile oxide |
| (VII)700647-3-a | 864736-87-8Available | 1,2,3-Trichloro-5-(3,3,3-trifluoroprop-1-en-2-yl)benzene |
| (VIII)700647-3-a | - | 3-Methyl-5-[5-(3,4,5-trichlorophenyl)-5-(trifluoromethyl)-4,5-dihydro-1,2-oxazol-3-yl]thiophene-2-carboxylic acid |
| (IX)700647-3-a | 1171331-39-7Available | 2-Amino-N-(2,2,2-trifluoroethyl)acetamide hydrochloride |
OptimisedRoute 8Steps 4 · Total yield /
(I)700647-4-a158401-00-4(II)700647-4-a859199-06-7(III)700647-4-a—(IV)700647-4-a—(V)700647-4-a1171331-39-7(VI)700647-4-a—(VII)700647-4-a7803-49-8API · Lotilaner
| Code | CAS No. | Intermediate |
|---|---|---|
| (I)700647-4-a | 158401-00-4Available | 2,2,2-Trifluoro-1-(3,4,5-trichlorophenyl)ethan-1-one |
| (II)700647-4-a | 859199-06-7Available | 1-(5-Bromo-4-methylthiophen-2-yl)ethan-1-one |
| (III)700647-4-a | - | 1-(5-Bromo-4-methylthiophen-2-yl)-4,4,4-trifluoro-3-(3,4,5-trichlorophenyl)but-2-en-1-one |
| (IV)700647-4-a | - | 3-Methyl-5-[4,4,4-trifluoro-3-(3,4,5-trichlorophenyl)but-2-enoyl]thiophene-2-carboxylic acid |
| (V)700647-4-a | 1171331-39-7Available | 2-Amino-N-(2,2,2-trifluoroethyl)acetamide hydrochloride |
| (VI)700647-4-a | - | 3-Methyl-N-[2-oxo-2-[(2,2,2-trifluoroethyl)amino]ethyl]-5-[4,4,4-trifluoro-3-(3,4,5-trichlorophenyl)but-2-enoyl]thiophene-2-carboxamide |
| (VII)700647-4-a | 7803-49-8Available | Amine N-oxide |
Frequently asked questions
What are the approved indications of Lotilaner?
Approved indications include: 蠕形螨性睑缘炎.
When does the Lotilaner patent expire?
No public expiry year is available for Lotilaner yet; this page updates once verified.
How many synthesis routes are recorded for Lotilaner?
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 Lotilaner intermediates?
39 intermediate CAS of Lotilaner 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 Lotilaner 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) · 2026-09-29