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Anacetrapib
Tier C — Watch / tradeAnacetrapib
MSD (Merck Sharp & Dohme)
Originator
-
First approval
-
Expiry (public)
No sales data
Peak sales
Small molecule
Type
Targets：HDL-cholesterol, CETP
Indications (approved)：Hypercholesterolaemia, Cardiac and vascular disorders, Dyslipidaemia, Atherosclerosis, Hyperlipoproteinaemia type II, Homozygous familial hypercholesterolaemia, Hyperlipidaemia, Coronary artery disease
Regional status
US
Phase III
2015-07-14
EU
Phase III
2011-06-01
China
Phase III
2014-10-22
Japan
-
Synthetic routes & intermediates5 routes
Originator routes × 1Optimised (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.
OriginatorRoute 1Steps 15 · Total yield 3.50 g
ANAC-001163444-17-5ANAC-0026526-08-5ANAC-003868166-20-5ANAC-004702641-04-1ANAC-005702641-05-2ANAC-006702641-06-3ANAC-007875444-08-9ANAC-008875446-35-8ANAC-009875446-29-0ANAC-010401-95-6ANAC-01179-24-3ANAC-0121152029-00-9ANAC-013875444-02-3ANAC-014—ANAC-01574457-86-6ANAC-01696826-25-4ANAC-0171262414-96-9ANAC-018944317-92-4API · Anacetrapib
| Code | CAS No. | Intermediate |
|---|---|---|
| ANAC-001 | 163444-17-5 | 2-iodo-4-(trifluoromethyl)aniline |
| ANAC-002 | 6526-08-5 | 2-amino-5-(trifluoromethyl)benzonitrile |
| ANAC-003 | 868166-20-5 | 2-iodo-5-(trifluoromethyl)benzonitrile |
| ANAC-004 | 702641-04-1 | 2-iodo-5-(trifluoromethyl)benzoic acid |
| ANAC-005 | 702641-05-2 | [2-iodo-5-(trifluoromethyl)phenyl]methanol |
| ANAC-006 | 702641-06-3 | 2-(bromomethyl)-1-iodo-4-(trifluoromethyl)benzene |
| ANAC-007 | 875444-08-9 | (4S,5R)-5-(3,5-bis(trifluoromethyl)phenyl)-4-methyloxazolidin-2-one |
| ANAC-008 | 875446-35-8 | (4S,5R)-5-(3,5-bis(trifluoromethyl)phenyl)-3-(2-iodo-5-(trifluoromethyl)benzyl)-4-methyloxazolidin-2-one |
| ANAC-009 | 875446-29-0 | (4-fluoro-5-isopropyl-2-methoxyphenyl)boronic acid |
| ANAC-010 | 401-95-6 | 3,5-bis(trifluoromethyl)benzaldehyde |
| ANAC-011 | 79-24-3 | nitroethane |
| ANAC-012 | 1152029-00-9 | 1-(3,5-bis(trifluoromethyl)phenyl)-2-nitropropan-1-ol |
| ANAC-013 | 875444-02-3 | 2-amino-1-(3,5-bis(trifluoromethyl)phenyl)propan-1-ol |
| ANAC-014 | - | 5-(3,5-bis(trifluoromethyl)phenyl)-4-methyloxazolidin-2-one |
| ANAC-015 | 74457-86-6 | 1-(2-fluoro-4-methoxyphenyl)ethan-1-one |
| ANAC-016 | 96826-25-4 | 2-(2-fluoro-4-methoxyphenyl)propan-2-ol |
| ANAC-017 | 1262414-96-9 | 2-fluoro-1-isopropyl-4-methoxybenzene |
| ANAC-018 | 944317-92-4 | 1-bromo-4-fluoro-5-isopropyl-2-methoxybenzene |
OptimisedRoute 2Steps 11 · Total yield 4.40 kg
ANAC-001163444-17-5ANAC-0026526-08-5ANAC-003868166-20-5ANAC-004702641-04-1ANAC-005702641-05-2ANAC-007875444-08-9ANAC-009875446-29-0ANAC-019875548-97-3ANAC-020875551-28-3ANAC-0211142-20-7ANAC-0221117-97-1ANAC-023114744-83-1ANAC-024114744-83-1ANAC-025871917-79-2ANAC-026877384-16-2API · Anacetrapib
| Code | CAS No. | Intermediate |
|---|---|---|
| ANAC-001 | 163444-17-5 | 2-iodo-4-(trifluoromethyl)aniline |
| ANAC-002 | 6526-08-5 | 2-amino-5-(trifluoromethyl)benzonitrile |
| ANAC-003 | 868166-20-5 | 2-iodo-5-(trifluoromethyl)benzonitrile |
| ANAC-004 | 702641-04-1 | 2-iodo-5-(trifluoromethyl)benzoic acid |
| ANAC-005 | 702641-05-2 | [2-iodo-5-(trifluoromethyl)phenyl]methanol |
| ANAC-007 | 875444-08-9 | (4S,5R)-5-(3,5-bis(trifluoromethyl)phenyl)-4-methyloxazolidin-2-one |
| ANAC-009 | 875446-29-0 | (4-fluoro-5-isopropyl-2-methoxyphenyl)boronic acid |
| ANAC-019 | 875548-97-3 | (4'-fluoro-5'-isopropyl-2'-methoxy-4-(trifluoromethyl)-[1,1'-biphenyl]-2-yl)methanol |
| ANAC-020 | 875551-28-3 | 2'-(chloromethyl)-4-fluoro-5-isopropyl-2-methoxy-4'-(trifluoromethyl)-1,1'-biphenyl |
| ANAC-021 | 1142-20-7 | (S)-2-(((benzyloxy)carbonyl)amino)propanoic acid |
| ANAC-022 | 1117-97-1Available | N,O-dimethylhydroxylamine |
| ANAC-023 | 114744-83-1 | 1-bromo-3,5-bis(trifluoromethyl)benzene |
| ANAC-024 | 114744-83-1 | 1-bromo-3,5-bis(trifluoromethyl)benzene |
| ANAC-025 | 871917-79-2 | benzyl (S)-(1-(3,5-bis(trifluoromethyl)phenyl)-1-oxopropan-2-yl)carbamate |
| ANAC-026 | 877384-16-2 | benzyl ((1R,2S)-1-(3,5-bis(trifluoromethyl)phenyl)-1-hydroxypropan-2-yl)carbamate |
OptimisedRoute 3Steps 9 · Total yield /
ANAC-018944317-92-4ANAC-019875548-97-3ANAC-020875551-28-3ANAC-027348-57-2ANAC-028450-88-4ANAC-02975-36-5ANAC-030914221-54-8ANAC-031958029-46-4ANAC-032851513-74-1ANAC-033958029-47-5ANAC-03479-22-1ANAC-035—API · Anacetrapib
| Code | CAS No. | Intermediate |
|---|---|---|
| ANAC-018 | 944317-92-4 | 1-bromo-4-fluoro-5-isopropyl-2-methoxybenzene |
| ANAC-019 | 875548-97-3 | (4'-fluoro-5'-isopropyl-2'-methoxy-4-(trifluoromethyl)-[1,1'-biphenyl]-2-yl)methanol |
| ANAC-020 | 875551-28-3 | 2'-(chloromethyl)-4-fluoro-5-isopropyl-2-methoxy-4'-(trifluoromethyl)-1,1'-biphenyl |
| ANAC-027 | 348-57-2 | 1-bromo-2,4-difluorobenzene |
| ANAC-028 | 450-88-4 | 1-bromo-4-fluoro-2-methoxybenzene |
| ANAC-029 | 75-36-5 | acetyl chloride |
| ANAC-030 | 914221-54-8 | 1-(5-bromo-2-fluoro-4-methoxyphenyl)ethan-1-one |
| ANAC-031 | 958029-46-4 | 2-(5-bromo-2-fluoro-4-methoxyphenyl)propan-2-ol |
| ANAC-032 | 851513-74-1 | 2-(3-(trifluoromethyl)phenyl)-4,5-dihydrooxazole |
| ANAC-033 | 958029-47-5 | 2-(4'-fluoro-5'-isopropyl-2'-methoxy-4-(trifluoromethyl)-[1,1'-biphenyl]-2-yl)-4,5-dihydrooxazole |
| ANAC-034 | 79-22-1 | methyl carbonochloridate |
| ANAC-035 | - | methyl (2-chloroethyl)(4'-fluoro-5'-isopropyl-2'-methoxy-4-(trifluoromethyl)-[1,1'-biphenyl]-2-carbonyl)carbamate |
OptimisedRoute 4Steps 9 · Total yield 4.50 g
ANAC-005702641-05-2ANAC-009875446-29-0ANAC-019875548-97-3ANAC-0211142-20-7ANAC-024114744-83-1ANAC-025871917-79-2ANAC-026877384-16-2ANAC-036875551-32-9ANAC-0371152029-16-7ANAC-0381620289-77-1ANAC-0391220703-07-0ANAC-040110-91-8ANAC-041376581-13-4API · Anacetrapib
| Code | CAS No. | Intermediate |
|---|---|---|
| ANAC-005 | 702641-05-2 | [2-iodo-5-(trifluoromethyl)phenyl]methanol |
| ANAC-009 | 875446-29-0 | (4-fluoro-5-isopropyl-2-methoxyphenyl)boronic acid |
| ANAC-019 | 875548-97-3 | (4'-fluoro-5'-isopropyl-2'-methoxy-4-(trifluoromethyl)-[1,1'-biphenyl]-2-yl)methanol |
| ANAC-021 | 1142-20-7 | (S)-2-(((benzyloxy)carbonyl)amino)propanoic acid |
| ANAC-024 | 114744-83-1 | 1-bromo-3,5-bis(trifluoromethyl)benzene |
| ANAC-025 | 871917-79-2 | benzyl (S)-(1-(3,5-bis(trifluoromethyl)phenyl)-1-oxopropan-2-yl)carbamate |
| ANAC-026 | 877384-16-2 | benzyl ((1R,2S)-1-(3,5-bis(trifluoromethyl)phenyl)-1-hydroxypropan-2-yl)carbamate |
| ANAC-036 | 875551-32-9 | 4'-fluoro-5'-isopropyl-2'-methoxy-4-(trifluoromethyl)-[1,1'-biphenyl]-2-carbaldehyde |
| ANAC-037 | 1152029-16-7 | (1R,2S)-2-amino-1-(3,5-bis(trifluoromethyl)phenyl)propan-1-ol |
| ANAC-038 | 1620289-77-1 | (1R,2S)-1-(3,5-bis(trifluoromethyl)phenyl)-2-(((E)-(4'-fluoro-5'-isopropyl-2'-methoxy-4-(trifluoromethyl)-[1,1'-biphenyl]-2-yl)methylene)amino)propan-1-ol |
| ANAC-039 | 1220703-07-0 | (1R,2S)-1-(3,5-bis(trifluoromethyl)phenyl)-2-(((4'-fluoro-5'-isopropyl-2'-methoxy-4-(trifluoromethyl)-[1,1'-biphenyl]-2-yl)methyl)amino)propan-1-ol |
| ANAC-040 | 110-91-8Available | morpholine |
| ANAC-041 | 376581-13-4 | benzyl (S)-(1-morpholino-1-oxopropan-2-yl)carbamate |
OptimisedRoute 5Steps 4 · Total yield 85.00 mg
ANAC-007875444-08-9ANAC-01179-24-3ANAC-020875551-28-3ANAC-04217352-25-9ANAC-0431480542-41-3ANAC-0441498289-59-0API · Anacetrapib
| Code | CAS No. | Intermediate |
|---|---|---|
| ANAC-007 | 875444-08-9 | (4S,5R)-5-(3,5-bis(trifluoromethyl)phenyl)-4-methyloxazolidin-2-one |
| ANAC-011 | 79-24-3 | nitroethane |
| ANAC-020 | 875551-28-3 | 2'-(chloromethyl)-4-fluoro-5-isopropyl-2-methoxy-4'-(trifluoromethyl)-1,1'-biphenyl |
| ANAC-042 | 17352-25-9 | 3,5-diiodobenzaldehyde |
| ANAC-043 | 1480542-41-3 | (1R,2S)-1-(3,5-diiodophenyl)-2-nitropropan-1-ol |
| ANAC-044 | 1498289-59-0 | (4S,5R)-5-(3,5-diiodophenyl)-4-methyloxazolidin-2-one |
Frequently asked questions
What are the approved indications of Anacetrapib?
Approved indications include: Hypercholesterolaemia, Cardiac and vascular disorders, Dyslipidaemia, Atherosclerosis, Hyperlipoproteinaemia type II, Homozygous familial hypercholesterolaemia, Hyperlipidaemia, Coronary artery disease.
When does the Anacetrapib patent expire?
No public expiry year is available for Anacetrapib yet; this page updates once verified.
How many synthesis routes are recorded for Anacetrapib?
5 synthesis routes are recorded; the shortest is 4 steps with 85.00 mg total yield. Intermediates in each route carry codes and CAS numbers.
Where can I buy Anacetrapib intermediates?
2 intermediate CAS of Anacetrapib 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 Anacetrapib 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