CAS 4318-56-3

6-chloro-3-methylpyrimidine-2,4(1H,3H)-dione

Codes: TREL-004, ALOG-021

Application context (from source-drug indications)

Type 2 diabetesTrelagliptin SuccinateDiabetesTrelagliptin SuccinateType 2 diabetesAlogliptin BenzoateDiabetesAlogliptin BenzoateAcute coronary syndromeAlogliptin Benzoate

Source drugs (routes using this intermediate)

Drug	Tier	Expiry
Trelagliptin Succinate	Tier C — Watch / trade	-
Alogliptin Benzoate	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.

Trelagliptin SuccinateOriginator routesteps: 9total yield: 1.546 kg

1-bromo-4-fluoro-2-methylbenzene→4-fluoro-2-methylbenzonitrile→2-(bromomethyl)-4-fluorobenzonitrile→6-chloro-3-methylpyrimidine-2,4(1H,3H)-dione→2-((6-chloro-3-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)methyl)-4-fluorobenzonitrile→(R)-piperidin-3-amine→succinic acid→(R)-2,5-diaminopentanoic acid hydrochloride→(R)-methyl 2,5-diaminopentanoate→(R)-3-aminopiperidin-2-one hydrochloride→(R)-piperidin-3-amine

Trelagliptin SuccinateOptimised routesteps: 4total yield: /

2-(bromomethyl)-4-fluorobenzonitrile→6-chloro-3-methylpyrimidine-2,4(1H,3H)-dione→2-((6-chloro-3-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)methyl)-4-fluorobenzonitrile→(R)-piperidin-3-amine→(R)-2-(piperidin-3-yl)isoindoline-1,3-dione→(R)-2-((6-(3-(1,3-dioxoisoindolin-2-yl)piperidin-1-yl)-3-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)methyl)-4-fluorobenzonitrile→isobenzofuran-1,3-dione

Alogliptin BenzoateOptimised routesteps: 5total yield: /

6-chloro-3-methylpyrimidine-2,4(1H,3H)-dione→(R)-tert-butyl (1-(3,5-dimethyl-2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridin-7-yl)piperidin-3-yl)carbamate→2-((6-chloro-3-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)methyl)benzonitrile→(R)-2-(piperidin-3-yl)isoindoline-1,3-dione→(R)-2-((6-(3-(1,3-dioxoisoindolin-2-yl)piperidin-1-yl)-3-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)methyl)benzonitrile→(R)-piperidin-3-amine dihydrochloride→isobenzofuran-1,3-dione

Intermediates available on this site

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Supplier	Product	Price band	MOQ	Lead time	Qualifications	Action
Unibest Nantong cGMP Site	6-Chloro-3-methyluracil Pharmaceutical Intermediates	On request	On request	On request	—

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