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CAS 372-09-8

2-cyanoacetic acidCyanoacetic acid

Codes: TOFA-028, TRAT-004, ALOG-017, AZEL-004, Urapidil-023, ENTA-004

Application context (from source-drug indications)

Ankylosing spondylitisTofacitinib CitrateJuvenile rheumatoid arthritisTofacitinib CitrateUlcerative colitisTofacitinib CitratePsoriatic arthritisTofacitinib CitrateRheumatoid arthritisTofacitinib CitrateThyroid cancerTrametinibGliomaTrametinibHairy cell leukaemiaTrametinibAnaplastic thyroid cancerTrametinibSolid tumourTrametinibNon-small cell lung cancerTrametinibType 2 diabetesAlogliptin BenzoateDiabetesAlogliptin BenzoateAcute coronary syndromeAlogliptin BenzoateHypertensionOlmesartan Medoxomil/AzelnidipineHypertensionAzelnidipineHypertensionUrapidil hydrochlorideParkinson's diseaseEntacapone立位耐力不良EntacaponeTachycardiaEntacaponeObesityEntacapone

Source drugs (routes using this intermediate)

DrugTierExpiry
Tofacitinib CitrateTier B — Position early2028
TrametinibTier C — Watch / trade2029
Alogliptin BenzoateTier C — Watch / trade-
Olmesartan Medoxomil/AzelnidipineTier C — Watch / trade-
AzelnidipineTier C — Watch / trade-
Urapidil hydrochlorideTier C — Watch / trade-
EntacaponeTier 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: 12total yield: 25 g
methyl (4-methylpyridin-3-yl)carbamate→4-methylpyridin-3-amine→methyl (4-methylpiperidin-3-yl)carbamate→methyl (4-methyl-1-tritylpiperidin-3-yl)carbamate→N,4-dimethyl-1-tritylpiperidin-3-amine hydrochloride→(3R,4R)-N,4-dimethyl-1-tritylpiperidin-3-amine (2R,3R)-2,3-bis((4-methylbenzoyl)oxy)succinate→(3R,4R)-N,4-dimethyl-1-tritylpiperidin-3-amine→2,4-dichloro-7-tosyl-7H-pyrrolo[2,3-d]pyrimidine→2-chloro-N-methyl-N-((3R,4R)-4-methyl-1-tritylpiperidin-3-yl)-7-tosyl-7H-pyrrolo[2,3-d]pyrimidin-4-amine→2-chloro-N-methyl-N-((3R,4R)-4-methyl-1-tritylpiperidin-3-yl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine→2-chloro-N-methyl-N-((3R,4R)-4-methylpiperidin-3-yl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine→2-cyanoacetic acid
Tofacitinib CitrateOptimised routesteps: 4total yield: 63.4 g
4-chloro-7H-pyrrolo[2,3-d]pyrimidine→2-cyanoacetic acid→tert-butyl methyl((3R,4R)-4-methylpiperidin-3-yl)carbamate→tert-butyl ((3R,4R)-1-(2-cyanoacetyl)-4-methylpiperidin-3-yl)(methyl)carbamate→3-((3R,4R)-4-methyl-3-(methylamino)piperidin-1-yl)-3-oxopropanenitrile
TrametinibOriginator routesteps: 10total yield: 8.3 g
2-fluoro-4-iodoaniline→cyclopropanamine→1-cyclopropyl-3-(2-fluoro-4-iodophenyl)urea→2-cyanoacetic acid→2-cyano-N-cyclopropyl-N-((2-fluoro-4-iodophenyl)carbamoyl)acetamide→6-amino-3-cyclopropyl-1-(2-fluoro-4-iodophenyl)pyrimidine-2,4(1H,3H)-dione→(E)-N'-(1-cyclopropyl-3-(2-fluoro-4-iodophenyl)-2,6-dioxo-1,2,3,6-tetrahydropyrimidin-4-yl)-N,N-dimethylformimidamide→3-cyclopropyl-1-(2-fluoro-4-iodophenyl)-6-(methylamino)pyrimidine-2,4(1H,3H)-dione→2-methylmalonic acid→3-cyclopropyl-1-(2-fluoro-4-iodophenyl)-5-hydroxy-6,8-dimethylpyrido[2,3-d]pyrimidine-2,4,7(1H,3H,8H)-trione→3-cyclopropyl-1-(2-fluoro-4-iodophenyl)-6,8-dimethyl-2,4,7-trioxo-1,2,3,4,7,8-hexahydropyrido[2,3-d]pyrimidin-5-yl 4-methylbenzenesulfonate→N-(3-aminophenyl)acetamide→N-(3-((3-cyclopropyl-1-(2-fluoro-4-iodophenyl)-6,8-dimethyl-2,4,7-trioxo-1,2,3,4,7,8-hexahydropyrido[2,3-d]pyrimidin-5-yl)amino)phenyl)acetamide
Alogliptin BenzoateOptimised routesteps: 5total yield: /
2-(aminomethyl)benzonitrile→1-(2-cyanobenzyl)-3-methylurea→2-cyanoacetic acid→2-cyano-N-((2-cyanobenzyl)carbamoyl)-N-methylacetamide→2-((6-amino-3-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)methyl)benzonitrile→tert-butyl (R)-piperidin-3-ylcarbamate hydrochloride→tert-butyl (R)-(1-(3-(2-cyanobenzyl)-1-methyl-2,6-dioxo-1,2,3,6-tetrahydropyrimidin-4-yl)piperidin-3-yl)carbamate
Olmesartan Medoxomil/AzelnidipineOriginator routesteps: 4total yield: 2.17 g
diphenylmethanamine→2-(chloromethyl)oxirane→1-benzhydrylazetidin-3-ol→2-cyanoacetic acid→1-benzhydrylazetidin-3-yl 2-cyanoacetate→1-benzhydrylazetidin-3-yl 3-amino-3-iminopropanoate acetate→isopropyl (E)-2-(3-nitrobenzylidene)-3-oxobutanoate
AzelnidipineOriginator routesteps: 4total yield: 2.17 g
diphenylmethanamine→2-(chloromethyl)oxirane→1-benzhydrylazetidin-3-ol→2-cyanoacetic acid→1-benzhydrylazetidin-3-yl 2-cyanoacetate→1-benzhydrylazetidin-3-yl 3-amino-3-iminopropanoate acetate→isopropyl (E)-2-(3-nitrobenzylidene)-3-oxobutanoate
Urapidil hydrochlorideOptimised routesteps: 2total yield: /
1,3-Dimethylurea→Cyanoacetic acid→Acetamide,2-cyano-N-methyl-N-[(methylamino)carbonyl]-→6-Amino-1,3-dimethyluracil
EntacaponeOptimised routesteps: 3total yield: 4.00 g
3,4-dihydroxy-5-nitrobenzaldehyde→2-cyanoacetic acid→(E)-2-cyano-3-(3,4-dihydroxy-5-nitrophenyl)acrylic acid→(E)-2-cyano-3-(3,4-dihydroxy-5-nitrophenyl)acryloyl chloride→diethylamine
EntacaponeOptimised routesteps: 3total yield: 9.45 g
3,4-dihydroxy-5-nitrobenzaldehyde→2-cyano-N,N-diethylacetamide→2-cyanoacetic acid→4-hydroxy-3-methoxy-5-nitrobenzaldehyde

Intermediates available on this site

Side-by-side comparison of all listed offers on this CAS; price bands are list-price ranges, final price subject to RFQ confirmation.

SupplierProductPrice bandMOQLead timeQualificationsAction
Unibest Nantong cGMP Site（3R,4R)-N,4-Dimethyl-1-(phenylmethyl)-3-piperidinamine HCL
Pharmaceutical Intermediates
On requestOn requestOn request
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Unibest Taizhou GMP-like Site4-Chloro-7-[(4-methylphenyl)sulfonyl]-7H-pyrrolo[2,3-d]pyrimidine
Pharmaceutical Intermediates
On requestOn requestOn request
—
Qualified Partner — East China API Works1-benzyl-4-methylpiperidin-3-one
Pharmaceutical Intermediates
On requestOn requestOn request
—
Unibest Nantong cGMP SiteN-methyl-N-((3R,4R)-4-methylpiperidin-3-yl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine
Pharmaceutical Intermediates
On requestOn requestOn request
—

This is a CAS-level registry record: registrations across routes are merged. Supplier offers and buyer demands will be matched on this CAS as the primary key.