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Itacitinib

Tier C — Watch / trade

Itacitinib

Incyte Corp
Originator
-
First approval
-
Expiry (public)
No sales data
Peak sales
Small molecule
Type

Targets:JAK2, JAK1

Indications (approved):Diffuse large B-cell lymphoma, Myeloproliferative neoplasm, Acute lymphoblastic leukaemia, Acute myeloid leukaemia, Chronic myelomonocytic leukaemia, 骨髓增生异常-骨髓增生性疾病, Myelofibrosis, 血小板增多

Regional status

US
Phase II
2012-03-01
EU
Phase II
2016-12-20
China
Discontinued
2020-06-18
Japan
Phase II
2020-08-03

Synthetic routes & intermediates2 routes

Originator routes × 1Optimised (non-patent) × 1Process 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 34.0 g
ITACI-00191-00-9ITACI-002106-89-8ITACI-00390604-02-7ITACI-004141699-55-0ITACI-005398489-26-4ITACI-0062537-48-6ITACI-0071153949-11-1ITACI-0081239322-61-2ITACI-0091153949-15-5ITACI-0103680-69-1ITACI-0111627504-41-9ITACI-0121627504-43-1ITACI-0131334303-99-9ITACI-01442899-11-6ITACI-015177-11-7ITACI-016886510-09-4ITACI-0171426436-72-7ITACI-018288-13-1ITACI-0193469-69-0ITACI-020189332-05-6ITACI-02161676-62-8Itacitinib1334298-90-6Itacitinib Adipate—API · Itacitinib
CodeCAS No.Intermediate
ITACI-00191-00-9diphenylmethanamine
ITACI-002106-89-82-(chloromethyl)oxirane
ITACI-00390604-02-71-benzhydrylazetidin-3-ol hydrochloride
ITACI-004141699-55-0tert-butyl 3-hydroxyazetidine-1-carboxylate
ITACI-005398489-26-4tert-butyl 3-oxoazetidine-1-carboxylate
ITACI-0062537-48-6diethyl (cyanomethyl)phosphonate
ITACI-0071153949-11-1tert-butyl 3-(cyanomethylene)azetidine-1-carboxylate
ITACI-0081239322-61-24-(4,4,5,5-tetramethyl-1,3-dioxolan-2-yl)-1H-pyrazole
ITACI-0091153949-15-5tert-butyl 3-(cyanomethyl)-3-(4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazol-1-yl)azetidine-1-carboxylate
ITACI-0103680-69-1Available4-chloro-7H-pyrrolo[2,3-d]pyrimidine
ITACI-0111627504-41-9tert-butyl 3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-3-(cyanomethyl)azetidine-1-carboxylate
ITACI-0121627504-43-12-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)azetidin-3-yl)acetonitrile dihydrochloride
ITACI-0131334303-99-91-(3-fluoro-2-(trifluoromethyl)isonicotinoyl)piperidin-4-one
ITACI-01442899-11-61,4-dioxa-8-azaspiro[4.5]decane hydrochloride
ITACI-015177-11-71,4-dioxa-8-azaspiro[4.5]decane
ITACI-016886510-09-43-fluoro-2-(trifluoromethyl)isonicotinic acid
ITACI-0171426436-72-7(3-fluoro-2-(trifluoromethyl)pyridin-4-yl)(1,4-dioxa-8-azaspiro[4.5]decan-8-yl)methanone
ITACI-018288-13-1Available1H-pyrazole
ITACI-0193469-69-0Available4-iodo-1H-pyrazole
ITACI-020189332-05-64-iodo-1-(trimethylsilyl)-1H-pyrazole
ITACI-02161676-62-82-isopropoxy-4,4,5,5-tetramethyl-1,3,2-dioxaborolane
Itacitinib1334298-90-62-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(1-(3-fluoro-2-(trifluoromethyl)isonicotinoyl)piperidin-4-yl)azetidin-3-yl)acetonitrile
Itacitinib Adipate-2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(1-(3-fluoro-2-(trifluoromethyl)isonicotinoyl)piperidin-4-yl)azetidin-3-yl)acetonitrile adipate
OptimisedRoute 2Steps 12 · Total yield 135 mg
ITACI-0071153949-11-1ITACI-0081239322-61-2ITACI-0103680-69-1ITACI-0131334303-99-9ITACI-018288-13-1ITACI-0221314910-43-4ITACI-0231627504-45-3ITACI-0241627504-47-5ITACI-0252075-45-8ITACI-0261024120-52-2ITACI-0271195-66-0ITACI-0281029716-44-6ITACI-0291193-24-4ITACI-0305305-40-8ITACI-03114160-93-1ITACI-0322092876-49-6Itacitinib1334298-90-6API · Itacitinib
CodeCAS No.Intermediate
ITACI-0071153949-11-1tert-butyl 3-(cyanomethylene)azetidine-1-carboxylate
ITACI-0081239322-61-24-(4,4,5,5-tetramethyl-1,3-dioxolan-2-yl)-1H-pyrazole
ITACI-0103680-69-1Available4-chloro-7H-pyrrolo[2,3-d]pyrimidine
ITACI-0131334303-99-91-(3-fluoro-2-(trifluoromethyl)isonicotinoyl)piperidin-4-one
ITACI-018288-13-1Available1H-pyrazole
ITACI-0221314910-43-42-(azetidin-3-ylidene)acetonitrile hydrochloride
ITACI-0231627504-45-32-(1-(1-(3-fluoro-2-(trifluoromethyl)isonicotinoyl)piperidin-4-yl)azetidin-3-ylidene)acetonitrile
ITACI-0241627504-47-52-(1-(1-(3-fluoro-2-(trifluoromethyl)isonicotinoyl)piperidin-4-yl)-3-(4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazol-1-yl)azetidin-3-yl)acetonitrile
ITACI-0252075-45-8Available4-bromo-1H-pyrazole
ITACI-0261024120-52-24-bromo-1-(1-ethoxyethyl)-1H-pyrazole
ITACI-0271195-66-02-methoxy-4,4,5,5-tetramethyl-1,3,2-dioxaborolane
ITACI-0281029716-44-6Available1-(1-ethoxyethyl)-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole
ITACI-0291193-24-4pyrimidine-4,6-diol
ITACI-0305305-40-84,6-dichloropyrimidine-5-carbaldehyde
ITACI-03114160-93-14-amino-6-chloropyrimidine-5-carbaldehyde
ITACI-0322092876-49-6(E)-6-chloro-5-(2-methoxyvinyl)pyrimidin-4-amine
Itacitinib1334298-90-62-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(1-(3-fluoro-2-(trifluoromethyl)isonicotinoyl)piperidin-4-yl)azetidin-3-yl)acetonitrile

Frequently asked questions

What are the approved indications of Itacitinib?

Approved indications include: Diffuse large B-cell lymphoma, Myeloproliferative neoplasm, Acute lymphoblastic leukaemia, Acute myeloid leukaemia, Chronic myelomonocytic leukaemia, 骨髓增生异常-骨髓增生性疾病, Myelofibrosis, 血小板增多.

When does the Itacitinib patent expire?

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

How many synthesis routes are recorded for Itacitinib?

2 synthesis routes are recorded; the shortest is 12 steps with 135 mg total yield. Intermediates in each route carry codes and CAS numbers.

Where can I buy Itacitinib intermediates?

5 intermediate CAS of Itacitinib 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 Itacitinib 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) · 2026-10-18