CAS 90213-66-4

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

Codes: TOFA-014, PF-06651600-007

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 tosylate

Source drugs (routes using this intermediate)

Drug	Tier	Expiry
Tofacitinib Citrate	Tier B — Position early	2028
Ritlecitinib tosylate	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

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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