CAS 90213-66-4

2,4-dichloro-7H-pyrrolo[2,3-d]pyrimidine

Codes: TOFA-014, PF-06651600-007, AVITI-001

Application context (from source-drug indications)

Ankylosing spondylitisTofacitinib CitrateJuvenile rheumatoid arthritisTofacitinib CitrateUlcerative colitisTofacitinib CitratePsoriatic arthritisTofacitinib CitrateRheumatoid arthritisTofacitinib CitrateAlopecia areataRitlecitinib tosylateVitiligoRitlecitinib tosylateChronic urticariaRitlecitinib tosylateHidradenitis suppurativaRitlecitinib tosylate瘢痕疙瘩Ritlecitinib tosylate乳糜泻Ritlecitinib tosylateNon-small cell lung cancerAbivertinibNon-Hodgkin lymphomaAbivertinibLymphomaAbivertinibChronic lymphocytic leukaemiaAbivertinibDiffuse large B-cell lymphomaAbivertinibMantle cell lymphomaAbivertinib

Source drugs (routes using this intermediate)

Drug	Tier	Expiry
Tofacitinib Citrate	Tier B — Position early	2028
Ritlecitinib tosylate	Tier C — Watch / trade	-
Abivertinib	Tier C — Watch / trade	-

Position in synthesis routes (up/downstream chain)

Ordered by route registration; left → right is the synthesis direction. The highlighted node is the current CAS; others link to their own profiles.

Tofacitinib CitrateOptimised routesteps: 7total yield: 42.85 g

(3R,4R)-1-benzyl-N,4-dimethylpiperidin-3-amine hemi((2R,3R)-2,3-bis((4-methylbenzoyl)oxy)succinate)→2,4-dichloro-7H-pyrrolo[2,3-d]pyrimidine→N-((3R,4R)-1-benzyl-4-methylpiperidin-3-yl)-2-chloro-N-methyl-7H-pyrrolo[2,3-d]pyrimidin-4-amine→1-benzyl-N,4-dimethylpiperidin-3-amine→N-methyl-N-(4-methylpiperidin-3-yl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine→ethyl 2-cyanoacetate→methyl (4-methylpyridin-3-yl)carbamate→1-benzyl-3-((methoxycarbonyl)amino)-4-methylpyridin-1-ium chloride→methyl (1-benzyl-4-methyl-1,2,5,6-tetrahydropyridin-3-yl)carbamate

Ritlecitinib tosylateOriginator routesteps: 9total yield: /

1-((2S,5R)-5-((7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)-2-methylpiperidin-1-yl)prop-2-en-1-one→6-methylpyridin-3-amine→tert-butyl (6-methylpyridin-3-yl)carbamate→tert-butyl (6-methylpiperidin-3-yl)carbamate→benzyl 5-((tert-butoxycarbonyl)amino)-2-methylpiperidine-1-carboxylate→(2S,5R)-benzyl 5-((tert-butoxycarbonyl)amino)-2-methylpiperidine-1-carboxylate→(2S,5R)-benzyl 5-amino-2-methylpiperidine-1-carboxylate→2,4-dichloro-7H-pyrrolo[2,3-d]pyrimidine→(2S,5R)-benzyl 5-((2-chloro-7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)-2-methylpiperidine-1-carboxylate→N-((3R,6S)-6-methylpiperidin-3-yl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine hydrochloride→1-((2S,5R)-5-((7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)-2-methylpiperidin-1-yl)prop-2-en-1-one

AbivertinibOriginator routesteps: 7total yield: /

2,4-dichloro-7H-pyrrolo[2,3-d]pyrimidine→2,4-dichloro-7-((2-(trimethylsilyl)ethoxy)methyl)-7H-pyrrolo[2,3-d]pyrimidine→3-nitrophenol→2-chloro-4-(3-nitrophenoxy)-7-((2-(trimethylsilyl)ethoxy)methyl)-7H-pyrrolo[2,3-d]pyrimidine→3-fluoro-4-(4-methylpiperazin-1-yl)aniline→N-(3-fluoro-4-(4-methylpiperazin-1-yl)phenyl)-4-(3-nitrophenoxy)-7-((2-(trimethylsilyl)ethoxy)methyl)-7H-pyrrolo[2,3-d]pyrimidin-2-amine→4-(3-aminophenoxy)-N-(3-fluoro-4-(4-methylpiperazin-1-yl)phenyl)-7-((2-(trimethylsilyl)ethoxy)methyl)-7H-pyrrolo[2,3-d]pyrimidin-2-amine→acryloyl chloride→N-(3-((2-((3-fluoro-4-(4-methylpiperazin-1-yl)phenyl)amino)-7-((2-(trimethylsilyl)ethoxy)methyl)-7H-pyrrolo[2,3-d]pyrimidin-4-yl)oxy)phenyl)acrylamide→N-(3-((2-((3-fluoro-4-(4-methylpiperazin-1-yl)phenyl)amino)-7-(hydroxymethyl)-7H-pyrrolo[2,3-d]pyrimidin-4-yl)oxy)phenyl)acrylamide

Intermediates available on this site

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Supplier	Product	Price band	MOQ	Lead time	Qualifications	Action
Unibest Nantong cGMP Site	2,4-dichloro-7H-pyrrolo[2,3-d]pyrimidine Pharmaceutical Intermediates	On request	On request	On request	—

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