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马来酸阿塞那平
Tier C — Watch / tradeAsenapine Maleate
默沙东
Originator
2009
First approval
-
Expiry (public)
$0.17B ▲
Peak sales
化学药
Type
Targets：5-HT2A、DRD2
Brand：Saphris、Sycrest
Indications (approved)：精神分裂症、躁狂症
Regional status
US
批准上市
2009-08-13
EU
批准上市
2010-09-01
China
临床一期
2022-07-11
Japan
批准上市
2016-03-28
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 6 · Total yield /
| Code | CAS No. | Intermediate |
|---|---|---|
| ASEN-001 | 70958-20-2 | 2-(5-chloro-2-phenoxyphenyl)acetic acid |
| ASEN-002 | 1428150-14-4 | 2-(5-chloro-2-phenoxyphenyl)acetyl chloride |
| ASEN-003 | 5473-12-1 | methyl methylglycinate |
| ASEN-004 | 1180843-76-8 | methyl N-(2-(5-chloro-2-phenoxyphenyl)acetyl)-N-methylglycinate |
| ASEN-005 | 1162120-35-5 | 3-(5-chloro-2-phenoxyphenyl)-1-methylpyrrolidine-2,4-dione |
| ASEN-006 | 1012884-46-6 | 11-chloro-2-methyl-2,3-dihydro-1H-dibenzo[2,3:6,7]oxepino[4,5-c]pyrrol-1-one |
| ASEN-007 | - | (3aR,12bR)-11-chloro-2-methyl-2,3,3a,12b-tetrahydro-1H-dibenzo[2,3:6,7]oxepino[4,5-c]pyrrol-1-one |
| ASEN-008 | - | (3aR,12bS)-11-chloro-2-methyl-2,3,3a,12b-tetrahydro-1H-dibenzo[2,3:6,7]oxepino[4,5-c]pyrrol-1-one |
OptimisedRoute 2Steps 4 · Total yield /
| Code | CAS No. | Intermediate |
|---|---|---|
| ASEN-011 | 635-93-8 | 5-chloro-2-hydroxybenzaldehyde |
| ASEN-014 | 1118-68-9 | dimethylglycine |
| ASEN-009-a | 3433-80-5 | 1-bromo-2-(bromomethyl)benzene |
| ASEN-009-b | - | 1-(chloromethyl)-2-iodobenzene |
| ASEN-009-c | 611-17-6 | 1-(bromomethyl)-2-chlorobenzene |
| ASEN-010-a | 63909-55-7 | diethyl (2-bromobenzyl)phosphonate |
| ASEN-010-b | 62680-68-6 | diethyl (2-iodobenzyl)phosphonate |
| ASEN-010-c | 29074-98-4 | diethyl (2-chlorobenzyl)phosphonate |
| ASEN-012-a | 1000889-96-2 | (E)-2-(2-bromostyryl)-4-chlorophenol |
| ASEN-012-b | 1000889-99-5 | (E)-4-chloro-2-(2-iodostyryl)phenol |
| ASEN-012-c | 1370255-96-1 | (E)-4-chloro-2-(2-chlorostyryl)phenol |
| ASEN-013-a | 1847487-55-1 | 2-((3S,4S)-4-(2-bromophenyl)-1-methylpyrrolidin-3-yl)-4-chlorophenol |
| ASEN-013-b | 1000890-00-5 | 4-chloro-2-((3S,4S)-4-(2-iodophenyl)-1-methylpyrrolidin-3-yl)phenol |
| ASEN-013-c | 1370255-92-7 | 4-chloro-2-((3S,4S)-4-(2-chlorophenyl)-1-methylpyrrolidin-3-yl)phenol |
OptimisedRoute 3Steps 4 · Total yield 44 g
| Code | CAS No. | Intermediate |
|---|---|---|
| ASEN-011 | 635-93-8 | 5-chloro-2-hydroxybenzaldehyde |
| ASEN-015 | - | - |
| ASEN-009-a | 3433-80-5 | 1-bromo-2-(bromomethyl)benzene |
| ASEN-010-a | 63909-55-7 | diethyl (2-bromobenzyl)phosphonate |
| ASEN-012-a | 1000889-96-2 | (E)-2-(2-bromostyryl)-4-chlorophenol |
| ASEN-013-a | 1847487-55-1 | 2-((3S,4S)-4-(2-bromophenyl)-1-methylpyrrolidin-3-yl)-4-chlorophenol |
OptimisedRoute 4Steps 9 · Total yield 9.3 g
| Code | CAS No. | Intermediate |
|---|---|---|
| ASEN-016 | 6630-33-7 | ethyl 4-(piperazin-1-yl)benzoate |
| ASEN-017 | 65185-68-4 | (E)-1-bromo-2-(2-nitrovinyl)benzene |
| ASEN-018 | 26939-01-5 | methyl 2-(5-chloro-2-methoxyphenyl)acetate |
| ASEN-019 | 1345459-05-3 | methyl 3-(2-bromophenyl)-2-(5-chloro-2-methoxyphenyl)-4-nitrobutanoate |
| ASEN-020 | 1345459-06-4 | 4-(2-bromophenyl)-3-(5-chloro-2-methoxyphenyl)pyrrolidin-2-one |
| ASEN-021 | 1345459-07-5 | 4-(2-bromophenyl)-3-(5-chloro-2-methoxyphenyl)-1-methylpyrrolidin-2-one |
| ASEN-022 | - | 3-(2-bromophenyl)-2-(5-chloro-2-methoxyphenyl)-4-(methylamino)butanoic acid |
| ASEN-023 | 1345459-09-7 | (3S,4S)-4-(2-bromophenyl)-3-(5-chloro-2-methoxyphenyl)-1-methylpyrrolidin-2-one |
| ASEN-024 | 1345459-10-0 | (3S,4S)-4-(2-bromophenyl)-3-(5-chloro-2-hydroxyphenyl)-1-methylpyrrolidin-2-one |
| ASEN-025 | 912356-08-2 | (3aS,12bS)-5-chloro-2-methyl-2,3,3a,12b-tetrahydro-1H-dibenzo[2,3:6,7]oxepino[4,5-c]pyrrol-1-one |
OptimisedRoute 5Steps 7 · Total yield 60 mg
| Code | CAS No. | Intermediate |
|---|---|---|
| ASEN-026 | 1141493-78-8 | methyl 2-(5-chloro-2-phenoxyphenyl)acetate |
| ASEN-027 | 553-90-2 | dimethyl oxalate |
| ASEN-028 | - | dimethyl 2-(5-chloro-2-phenoxyphenyl)-3-oxosuccinate |
| ASEN-029 | 1037313-26-0 | 5-chlorodibenzo[b,f]furo[3,4-d]oxepine-1,3-dione |
| ASEN-030 | 1037313-28-2 | dimethyl 2-chlorodibenzo[b,f]oxepine-10,11-dicarboxylate |
| ASEN-031 | 1037313-30-6 | dimethyl (10S,11S)-2-chloro-10,11-dihydrodibenzo[b,f]oxepine-10,11-dicarboxylate |
| ASEN-032 | 1037313-32-8 | ((10S,11S)-2-chloro-10,11-dihydrodibenzo[b,f]oxepine-10,11-diyl)dimethanol |
| ASEN-033 | 1037313-33-9 | ((10S,11S)-2-chloro-10,11-dihydrodibenzo[b,f]oxepine-10,11-diyl)bis(methylene) dimethanesulfonate |
Frequently asked questions
What are the approved indications of Asenapine Maleate?
Approved indications include: 精神分裂症, 躁狂症.
When does the Asenapine Maleate patent expire?
No public expiry year is available for Asenapine Maleate yet; this page updates once verified.
How many synthesis routes are recorded for Asenapine Maleate?
5 synthesis routes are recorded; the shortest is 4 steps with / total yield. Intermediates in each route carry codes and CAS numbers.
Where can I buy Asenapine Maleate intermediates?
All intermediates in Asenapine Maleate routes have CAS profiles — you can submit an RFQ per CAS and it enters the Unibest matching pool.
How do I get a quote for Asenapine Maleate 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