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Tofacitinib Citrate

Tier B — Position early

Tofacitinib Citrate · all drugs expiring in 2028 →

Pfizer Inc.
Originator
2012
First approval
2028
Expiry (public)
$2.46B ▲
Peak sales
Small molecule
Type

Targets：JAK1, JAK2, JAK3

Brand：Xeljanz, Jakvinus

Indications (approved)：Ankylosing spondylitis, Juvenile rheumatoid arthritis, Ulcerative colitis, Psoriatic arthritis, Rheumatoid arthritis

Regional status

US
Approved
2012-11-06
EU
Approved
2017-03-21
China
Approved
2017-03-10
Japan
Approved
2013-03-25

Factories producing this API1

Factories registered as producing this API in our sourcing network (RFQ records + product master), sorted by RFQ activity; the snapshot carries no cost or customer data.

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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: Ankylosing spondylitis, Juvenile rheumatoid arthritis, Ulcerative colitis, Psoriatic arthritis, Rheumatoid arthritis.

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) · 2026-09-29