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马来酸阿法替尼

Tier C — Watch / trade

Afatinib Dimaleate

勃林格殷格翰
Originator
2013
First approval
-
Expiry (public)
No sales data
Peak sales
化学药
Type

TargetsHER4、EGFR、HER2、EGFR L858R、EGFR 19del

BrandGiotrif、Tovok、Tomtovok、吉泰瑞、Gilotrif

Indications (approved)非小细胞肺癌

Regional status

US
批准上市
2013-07-12
EU
批准上市
2013-09-25
China
批准上市
2017-02-21
Japan
批准上市
2014-01-17

Synthetic routes & intermediates4 routes

Originator routes × 2Optimised (non-patent) × 2Process 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 /
Synthetic routes & intermediates Route 1
CodeCAS No.Intermediate
AFAT-0011194097-41-02-amino-4-fluoro-5-nitrobenzoic acid
AFAT-002162012-69-3N-(4-((3-chloro-4-fluorophenyl)(3,4-dimethoxybenzyl)amino)-7-(3-morpholinopropoxy)quinazolin-6-yl)acrylamide
AFAT-003162012-70-63-chloro-N-(3,4-dimethoxybenzyl)-4-fluoroaniline
AFAT-004367-21-53-chloro-4-fluoroaniline
AFAT-005162012-67-1AvailableN-(3-chloro-4-fluorophenyl)-7-fluoro-6-nitroquinazolin-4-amine
AFAT-00686087-23-2Available(S)-tetrahydrofuran-3-ol
AFAT-007314771-88-5(S)-N-(3-chloro-4-fluorophenyl)-6-nitro-7-((tetrahydrofuran-3-yl)oxy)quinazolin-4-amine
AFAT-008314771-76-1(S)-N4-(3-chloro-4-fluorophenyl)-7-((tetrahydrofuran-3-yl)oxy)quinazoline-4,6-diamine
AFAT-00913991-36-1(E)-4-bromobut-2-enoic acid
OriginatorRoute 2Steps 9 · Total yield 8.11 kg
Synthetic routes & intermediates Route 2
CodeCAS No.Intermediate
AFAT-004367-21-53-chloro-4-fluoroaniline
AFAT-00686087-23-2Available(S)-tetrahydrofuran-3-ol
AFAT-007314771-88-5(S)-N-(3-chloro-4-fluorophenyl)-6-nitro-7-((tetrahydrofuran-3-yl)oxy)quinazolin-4-amine
AFAT-008314771-76-1(S)-N4-(3-chloro-4-fluorophenyl)-7-((tetrahydrofuran-3-yl)oxy)quinazoline-4,6-diamine
AFAT-010-2-amino-4-chlorobenzoic acid
AFAT-01131374-18-27-chloroquinazolin-4(3H)-one
AFAT-01253449-14-27-chloro-6-nitroquinazolin-4(4aH)-one
AFAT-013162012-71-74,7-dichloro-6-nitroquinazoline
AFAT-014945553-94-6N-(3-chloro-4-fluorophenyl)-6-nitro-7-(phenylsulfonyl)quinazolin-4-amine
AFAT-0153095-95-22-(diethoxyphosphoryl)acetic acid
AFAT-016618061-76-0(S)-diethyl (2-((4-((3-chloro-4-fluorophenyl)amino)-7-((tetrahydrofuran-3-yl)oxy)quinazolin-6-yl)amino)-2-oxoethyl)phosphonate
AFAT-0173616-56-62,2-diethoxy-N,N-dimethylethanamine
AFAT-018110-16-7Availablemaleic acid
OptimisedRoute 3Steps 7 · Total yield 1.15 g
Synthetic routes & intermediates Route 3
CodeCAS No.Intermediate
AFAT-004367-21-53-chloro-4-fluoroaniline
AFAT-00686087-23-2Available(S)-tetrahydrofuran-3-ol
AFAT-019536-25-4methyl 3-amino-4-hydroxybenzoate
AFAT-0201454655-89-0methyl 5-amino-4-hydroxy-2-nitrobenzoate
AFAT-0211454656-00-8methyl 2,5-diamino-4-hydroxybenzoate
AFAT-0221156986-96-76-amino-7-hydroxyquinazolin-4(3H)-one
AFAT-0231451008-28-86-amino-4-chloroquinazolin-7-ol
AFAT-0241451008-29-9(S)-4-chloro-7-((tetrahydrofuran-3-yl)oxy)quinazolin-6-amine
AFAT-0251056149-69-9(E)-4-(dimethylamino)but-2-enoyl chloride
AFAT-0261451008-30-2(S,E)-N-(4-chloro-7-((tetrahydrofuran-3-yl)oxy)quinazolin-6-yl)-4-(dimethylamino)but-2-enamide
OptimisedRoute 4Steps 8 · Total yield 12.4 g
Synthetic routes & intermediates Route 4
CodeCAS No.Intermediate
AFAT-004367-21-53-chloro-4-fluoroaniline
AFAT-00686087-23-2Available(S)-tetrahydrofuran-3-ol
AFAT-0251056149-69-9(E)-4-(dimethylamino)but-2-enoyl chloride
AFAT-027767-00-04-hydroxybenzonitrile
AFAT-0283272-08-0Available4-hydroxy-3-nitrobenzonitrile
AFAT-0291451012-56-8(S)-3-nitro-4-((tetrahydrofuran-3-yl)oxy)benzonitrile
AFAT-0301451012-57-9(S)-3-amino-4-((tetrahydrofuran-3-yl)oxy)benzonitrile
AFAT-0311637330-92-7(S,E)-N-(5-cyano-2-((tetrahydrofuran-3-yl)oxy)phenyl)-4-(dimethylamino)but-2-enamide
AFAT-0321637330-93-8(S,E)-N-(5-cyano-4-nitro-2-((tetrahydrofuran-3-yl)oxy)phenyl)-4-(dimethylamino)but-2-enamide
AFAT-0331451369-97-3(S,E)-N-(4-amino-5-cyano-2-((tetrahydrofuran-3-yl)oxy)phenyl)-4-(dimethylamino)but-2-enamide
AFAT-0341451369-98-4(E)-N-(5-cyano-4-((E)-((dimethylamino)methylene)amino)-2-(((S)-tetrahydrofuran-3-yl)oxy)phenyl)-4-(dimethylamino)but-2-enamide

Frequently asked questions

What are the approved indications of Afatinib Dimaleate?

Approved indications include: 非小细胞肺癌.

When does the Afatinib Dimaleate patent expire?

No public expiry year is available for Afatinib Dimaleate yet; this page updates once verified.

How many synthesis routes are recorded for Afatinib Dimaleate?

4 synthesis routes are recorded; the shortest is 6 steps with / total yield. Intermediates in each route carry codes and CAS numbers.

Where can I buy Afatinib Dimaleate intermediates?

4 intermediate CAS of Afatinib Dimaleate 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 Afatinib Dimaleate 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