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枸橼酸托法替布

Tier B — Position early

Tofacitinib Citrate · all drugs expiring in 2028 →

辉瑞
Originator
2012
First approval
2028
Expiry (public)
$2.46B ▲
Peak sales
化学药
Type

Targets：JAK1、JAK2、JAK3

Brand：Xeljanz、尚杰、安舒正、Jakvinus

Indications (approved)：强直性脊柱炎、幼年型类风湿性关节炎、溃疡性结肠炎、银屑病关节炎、类风湿关节炎

Regional status

US
批准上市
2012-11-06
EU
批准上市
2017-03-21
China
批准上市
2017-03-10
Japan
批准上市
2013-03-25

Synthetic routes & intermediates7 routes

Originator routes × 1Optimised (non-patent) × 5Process routes × 1

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 4 · Total yield /
Synthetic routes & intermediates Route 1
CodeCAS No.Intermediate
TOFA-00132018-96-5Available1-benzyl-4-methylpiperidin-3-one
TOFA-002384338-23-2Available1-benzyl-N,4-dimethylpiperidin-3-amine
TOFA-0033680-69-1Available4-chloro-7H-pyrrolo[2,3-d]pyrimidine
TOFA-004384337-90-0AvailableN-(1-benzyl-4-methylpiperidin-3-yl)-N-methyl-7H-pyrrolo[2,3-d]pyrimidin-4-amine
TOFA-005384336-73-6AvailableN-methyl-N-(4-methylpiperidin-3-yl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine
TOFA-00616130-58-8Available2-cyanoacetyl chloride
OptimisedRoute 3Steps 7 · Total yield 42.85 g
Synthetic routes & intermediates Route 3
CodeCAS No.Intermediate
TOFA-013477600-71-8Available(3R,4R)-1-benzyl-N,4-dimethylpiperidin-3-amine hemi((2R,3R)-2,3-bis((4-methylbenzoyl)oxy)succinate)
TOFA-01490213-66-4Available2,4-dichloro-7H-pyrrolo[2,3-d]pyrimidine
TOFA-015923036-25-3AvailableN-((3R,4R)-1-benzyl-4-methylpiperidin-3-yl)-2-chloro-N-methyl-7H-pyrrolo[2,3-d]pyrimidin-4-amine
TOFA-002384338-23-2Available1-benzyl-N,4-dimethylpiperidin-3-amine
TOFA-005384336-73-6AvailableN-methyl-N-(4-methylpiperidin-3-yl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine
TOFA-009105-56-6Availableethyl 2-cyanoacetate
TOFA-010694495-63-1Availablemethyl (4-methylpyridin-3-yl)carbamate
TOFA-011923036-29-7Available1-benzyl-3-((methoxycarbonyl)amino)-4-methylpyridin-1-ium chloride
TOFA-012923036-28-6Availablemethyl (1-benzyl-4-methyl-1,2,5,6-tetrahydropyridin-3-yl)carbamate
OptimisedRoute 4Steps 5 · Total yield 1.1 g
Synthetic routes & intermediates Route 4
CodeCAS No.Intermediate
TOFA-002384338-23-2Available1-benzyl-N,4-dimethylpiperidin-3-amine
TOFA-0033680-69-1Available4-chloro-7H-pyrrolo[2,3-d]pyrimidine
TOFA-004384337-90-0AvailableN-(1-benzyl-4-methylpiperidin-3-yl)-N-methyl-7H-pyrrolo[2,3-d]pyrimidin-4-amine
TOFA-005384336-73-6AvailableN-methyl-N-(4-methylpiperidin-3-yl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine
TOFA-013477600-71-8Available(3R,4R)-1-benzyl-N,4-dimethylpiperidin-3-amine hemi((2R,3R)-2,3-bis((4-methylbenzoyl)oxy)succinate)
TOFA-0161228879-37-5Available1-benzyl-N,4-dimethylpiperidin-3-amine dihydrochloride
TOFA-01756657-76-2Available2,5-dioxopyrrolidin-1-yl 2-cyanoacetate
OptimisedRoute 5Steps 12 · Total yield 25 g
Synthetic routes & intermediates Route 5
CodeCAS No.Intermediate
TOFA-010694495-63-1Availablemethyl (4-methylpyridin-3-yl)carbamate
TOFA-0183430-27-1Available4-methylpyridin-3-amine
TOFA-0191204176-45-3Availablemethyl (4-methylpiperidin-3-yl)carbamate
TOFA-0201616760-91-8Availablemethyl (4-methyl-1-tritylpiperidin-3-yl)carbamate
TOFA-021-N,4-dimethyl-1-tritylpiperidin-3-amine hydrochloride
TOFA-0221616761-04-6Available(3R,4R)-N,4-dimethyl-1-tritylpiperidin-3-amine (2R,3R)-2,3-bis((4-methylbenzoyl)oxy)succinate
TOFA-0231616760-93-0Available(3R,4R)-N,4-dimethyl-1-tritylpiperidin-3-amine
TOFA-024934524-10-4Available2,4-dichloro-7-tosyl-7H-pyrrolo[2,3-d]pyrimidine
TOFA-0251616760-94-1Available2-chloro-N-methyl-N-((3R,4R)-4-methyl-1-tritylpiperidin-3-yl)-7-tosyl-7H-pyrrolo[2,3-d]pyrimidin-4-amine
TOFA-0261616760-96-3Available2-chloro-N-methyl-N-((3R,4R)-4-methyl-1-tritylpiperidin-3-yl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine
TOFA-0271616760-97-4Available2-chloro-N-methyl-N-((3R,4R)-4-methylpiperidin-3-yl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine
TOFA-028372-09-8Available2-cyanoacetic acid
OptimisedRoute 6Steps 5 · Total yield 23.6 g
Synthetic routes & intermediates Route 6
CodeCAS No.Intermediate
TOFA-004384337-90-0AvailableN-(1-benzyl-4-methylpiperidin-3-yl)-N-methyl-7H-pyrrolo[2,3-d]pyrimidin-4-amine
TOFA-005384336-73-6AvailableN-methyl-N-(4-methylpiperidin-3-yl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine
TOFA-00616130-58-8Available2-cyanoacetyl chloride
TOFA-029108-89-4Available4-methylpyridine
TOFA-03032018-56-7Available1-benzyl-4-methyl-1,2,3,6-tetrahydropyridine
TOFA-03158878-98-1Available(3S,4R)-1-benzyl-4-methylpiperidin-3-ol
TOFA-03278727-16-9AvailableN-methyl-7H-pyrrolo[2,3-d]pyrimidin-4-amine
OptimisedRoute 7Steps 4 · Total yield 63.4 g
Synthetic routes & intermediates Route 7
CodeCAS No.Intermediate
TOFA-0033680-69-1Available4-chloro-7H-pyrrolo[2,3-d]pyrimidine
TOFA-028372-09-8Available2-cyanoacetic acid
TOFA-0331206824-89-6Availabletert-butyl methyl((3R,4R)-4-methylpiperidin-3-yl)carbamate
TOFA-0341629858-77-0Availabletert-butyl ((3R,4R)-1-(2-cyanoacetyl)-4-methylpiperidin-3-yl)(methyl)carbamate
TOFA-0351629858-78-1Available3-((3R,4R)-4-methyl-3-(methylamino)piperidin-1-yl)-3-oxopropanenitrile
ProcessRoute 2Steps 5 · Total yield 2.08 kg
Synthetic routes & intermediates Route 2
CodeCAS No.Intermediate
TOFA-002384338-23-2Available1-benzyl-N,4-dimethylpiperidin-3-amine
TOFA-0033680-69-1Available4-chloro-7H-pyrrolo[2,3-d]pyrimidine
TOFA-004384337-90-0AvailableN-(1-benzyl-4-methylpiperidin-3-yl)-N-methyl-7H-pyrrolo[2,3-d]pyrimidin-4-amine
TOFA-005384336-73-6AvailableN-methyl-N-(4-methylpiperidin-3-yl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine
TOFA-0071639406-86-2Available4-chloro-7-(methylsulfonyl)-7H-pyrrolo[2,3-d]pyrimidine
TOFA-0081639406-87-3AvailableN-((3R,4R)-1-benzyl-4-methylpiperidin-3-yl)-N-methyl-7-(methylsulfonyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine
TOFA-009105-56-6Availableethyl 2-cyanoacetate

Frequently asked questions

What are the approved indications of Tofacitinib Citrate?

Approved indications include: 强直性脊柱炎, 幼年型类风湿性关节炎, 溃疡性结肠炎, 银屑病关节炎, 类风湿关节炎.

When does the Tofacitinib Citrate patent expire?

Based on public sources, the Tofacitinib Citrate patent expires in 2028.

How many synthesis routes are recorded for Tofacitinib Citrate?

7 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 Tofacitinib Citrate intermediates?

34 intermediate CAS of Tofacitinib Citrate 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 Tofacitinib Citrate 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