337519-92-3

Basic information

• Product Name: ethyl N-[4-(1-t-butoxycarbonylpiperidin-4-yloxy)-3-methylphenyl]sulfamoylacetate
• Synonyms: ethyl N-[4-(1-t-butoxycarbonylpiperidin-4-yloxy)-3-methylphenyl]sulfamoylacetate
• CAS NO: 337519-92-3
• Molecular Weight: 456.56
• Mol File: 337519-92-3.mol

Chemical Properties

• CAS DataBase Reference: ethyl N-[4-(1-t-butoxycarbonylpiperidin-4-yloxy)-3-methylphenyl]sulfamoylacetate(CAS DataBase Reference)
• NIST Chemistry Reference: ethyl N-[4-(1-t-butoxycarbonylpiperidin-4-yloxy)-3-methylphenyl]sulfamoylacetate(337519-92-3)
• EPA Substance Registry System: ethyl N-[4-(1-t-butoxycarbonylpiperidin-4-yloxy)-3-methylphenyl]sulfamoylacetate(337519-92-3)

Safety Data

• Hazardous Substances Data: 337519-92-3(Hazardous Substances Data)

Upstream product

• 138227-69-7 1-tert-butyloxycarbonyl-4-(4-amino-2-methylphenyloxy)piperidine 
• 55896-93-0 ethyl 2-(chlorosulfonyl)acetate 
• 141-78-6 ethyl acetate 

Downstream Products

• 337521-73-0 ethyl N-[4-(1-t-butoxycarbonylpiperidin-4-yloxy)-3-methylphenyl]-N-[3-(3-cyanophenyl)-2-(E)-propenyl]sulfamoylacetate 

Relevant articles and documents

Cinnamyl derivatives: Synthesis and factor Xa (FXa) inhibitory activities

To develop a potent and oral anticoagulant, a series of compounds with cinnamyl moiety was synthesized and their factor Xa (FXa) inhibitory activities were examined. As a result, some cinnamyl derivatives showed potent FXa inhibitory activities in vitro. Among them, compounds with substituent at the 3-position on the central benzene ring represented by (N-{4-[1-(acetimidoyl) piperidin-4-yloxy]-3-chlorophenyl}-N-[(E)-3-(3-amidinophenyl)-2-propenyl] sulfamoyl)acetic acid dihydrochloride (45b) and (N-{4-[1-(acetimidoyl)piperidin- 4-yloxy]-3-carbamoylphenyl}-N-[(E)-3-(3-amidinophenyl)-2-propenyl]sulfamoyl) acetic acid dihydrochloride (45j) exhibited potent FXa inhibitory activities with IC50 values of less than 10 nM in vitro. These compounds also showed potent anticoagulant activities both in vitro and ex vivo. Furthermore, these compounds exhibited no lethal toxicity (30 mg/kg, i.v.).

BENZAMIDINE DERIVATIVE

Compounds of general formula (1) and pharmacologically acceptable salts thereof: ???[wherein ??????R1 represents a hydrogen atom, a halogen atom, an alkyl group or a hydroxyl group; ??????R2 represents a hydrogen atom or a halogen atom; ??????R3 represents a hydrogen atom, an alkyl group which may be substituted, an aralkyl group, an alkylcarbonyl group which may be substituted, an alkylsulfonyl group which may be substituted or the like; ??????each of R4 and R5 represents a hydrogen atom, a halogen atom, an alkyl group which may be substituted, a carbamoyl group or the like; ??????R6 represents a heterocycle or the like; ??????each of R7 and R8 represents a hydrogen atom, an alkyl group or the like; ??????n represents 0, 1 or 2] ???exhibit excellent activated blood coagulation factor X inhibitory activity and are useful for the prevention or treatment of blood coagulation-related diseases.

BENZAMIDINE DERIVATIVES

Benzamidine derivatives of formula (I) or pharmaceutically acceptable salts thereof exhibit excellent inhibitory activity against factor Xa and are useful for treating or preventing blood coagulation disorders: wherein R 1represents a hydrogen atom, a halogen atom, an alkyl group or a hydroxyl group; R 2represents a hydrogen atom, a halogen atom or an alkyl group, R 3represents a hydrogen atom, an optionally substituted alkyl group, an aralkyl group, an optionally substituted alkanoyl group or an optionally substituted alkylsulfonyl group, R 4and R 5 are the same as or different from each other and each represent a hydrogen atom, a halogen atom, an optionally substituted alkyl group, an alkoxy group, a carboxyl group, an alkoxycarbonyl group or an optionally substituted carbamoyl group, and R 6represents a substituted pyrrolidine group or substituted piperidine group.