720720-96-7

Basic information

• Product Name: 5-Methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine-2-carboxylic acid hydrochloride
• Synonyms: 4,5,6,7-tetrahydro-5-Methyl-Thiazolo[5,4-c]pyridine-2-carboxylic acid hydrochloride;5-Methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine-2-carboxylic acid hydrochloride;EthanediaMide iMpurity B HCL;Thiazolo[5,4-c]pyridine-2-carboxylic acid, 4,5,6,7-tetrahydro-5-Methyl-, hydrochloride (1:1);5-Methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine-2-carboxylic acid hydrochloride(for Edoxaban);5-methyl-4H,5H,6H,7H-[1,3]thiazolo[5,4-c]pyridine-2-carboxylic acid hydrochloride;4,5,6,7-tetrahydro-5-Methyl-Thiazolo[5,4-c]pyridin;4,5,6,7-tetrahydro-5-Methyl-Thiazolo[5,4-c]pyridine-2-carboxylic acid HCl
• CAS NO: 720720-96-7
• Molecular Formula: C₈H₁₀N₂O₂S*ClH
• Molecular Weight: 234.7
• EINECS: 1592732-453-0
• Mol File: 720720-96-7.mol
• Article Data: 6

Chemical Properties

• Melting Point: 199.0 to 203.0 °C
• Boiling Point: 175℃[at 101 325 Pa]
• Appearance: /
• Storage Temp.: under inert gas (nitrogen or Argon) at 2-8°C
• Solubility: Aqueous Acid (Slightly), DMSO (Slightly, Heated, Sonicated), Methanol (Very Slig
• Stability: Hygroscopic
• CAS DataBase Reference: 5-Methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine-2-carboxylic acid hydrochloride(CAS DataBase Reference)
• NIST Chemistry Reference: 5-Methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine-2-carboxylic acid hydrochloride(720720-96-7)
• EPA Substance Registry System: 5-Methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine-2-carboxylic acid hydrochloride(720720-96-7)

Safety Data

• Hazardous Substances Data: 720720-96-7(Hazardous Substances Data)

Usage

Uses

5-Methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine-2-carboxylic Acid Hydrochloride is used as a reagent in the synthesis of N-(2-acylaminobenzyl or 2-acylaminoheterocyclylmethyl)thiophene-2-carboxamide derivatives as antithrombotics. It is also used as a reagent in the synthesis of diamide derivatives as FXa inhibitors. 5-Methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine-2-carboxylic Acid Hydrochloride is an intermediate for Edoxaban (E555520).

Upstream product

• 852291-42-0 2-bromo-5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine p-toluenesulfonate 
• 124-38-9 carbon dioxide 
• 259809-24-0 5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine 
• 143150-92-9 2-Bromo-5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]-pyridine 
• 89580-42-7 3-bromo-1-methylpiperidin-4-one hydrobromide 
• 76-02-8 trifluoroacetyl chloride 
• 1864-94-4 phenyl formate 
• 1445-73-4 1-Methyl-4-piperidone 

Downstream Products

• 480449-70-5 edoxaban 
• 480449-71-6 [14C]-Edoxaban tosylate 
• 912273-65-5 N₁-(5-chloropyridin-2-yl)-N₂-{(1S,2S,4R)-4-(dimethylaminocarbonyl)-2-[(5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridin-2-yl)carboxamido]cyclohexyl}oxalamide p-toluenesulfonic acid 
• 912273-65-5 N₁-(5-chloropyridin-2-yl)-N₂-{(1R,2S,4R)-4-(dimethylaminocarbonyl)-2-[(5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridin-2-yl)carboxamido]cyclohexyl}oxalamide p-toluenesulfonic acid 
• 912273-65-5 N₁-(5-chloropyridin-2-yl)-N₂-{(1R,2R,4S)-4-(dimethylaminocarbonyl)-2-[(5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridin-2-yl)carboxamido]cyclohexyl}oxalamide p-toluenesulfonic acid 
• 1057651-77-0 C₂₀H₂₆N₄O₃S 
• 1286182-25-9 N-(2-nitrobenzyl)-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide 
• 1286182-04-4 N-(2-{[(5-chlorothiophen-2-yl)carbonyl]amino}benzyl)-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide hydrochloride 
• 1286182-20-4 N-(2-{[(5-chlorothiophen-2-yl)carbonyl]amino}benzyl)-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide 
• 1057650-46-0 N-(2-{[(5-chlorothiophen-2-yl)carbonylamino]methyl}phenyl)-5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide 
• 480449-70-5 N₁-(5-chloropyridin-2-yl)-N₂-{(1SR,2RS,4SR)-4-(dimethylcarbamoyl)-2-[(5-methyl-4,5,6,7-tetrahydro [1,3]thiazolo[5,4-c]pyridine-2-carbonyl)amino]cyclohexyl}ethanediamide 

Relevant articles and documents

Method for preparing edoxaban from trichloroacetophenone onium salt derivatives

The invention provides a method for preparing edoxaban by using 2, 2, 2-trichloro-1-(4, 5, 6, 7-tetrahydro-5-methylthiazolo[5, 4-c]pyridinium-1-yl) ethanone chloride. The preparation method comprisesthe following steps: preparing 2, 2, 2-trichloro-1-(4, 5, 6, 7-tetrahydro-5-methylthiazolo[5, 4-c]pyridinium-1-yl) ethanone chloride, namely 109C5-11; the invention discloses a preparation method of N1[(1S, 2R, 4S)-2-amino-4-[(dimethylamino) carbonyl]cyclohexyl]-N2(5-chloro-2-pyridyl) oxalamide dimesylate, namely 109T2-31. The 109C5-11 is used as an acylation reagent to prepare the edoxaban with 109T2-31. The preparation method comprises the following steps: preparing the edoxaban by using the 109C5-11 as the acylation reagent; the novel method overcomes the defect that expensive condensing agents EDCI.HCl and activating agents HOBt need to be used in the prior art. The new method provided by the invention is beneficial to more economically and more efficiently realizing industrial scale production of the Edoxaban p-toluenesulfonate hydrate.

METHOD FOR PRODUCING INHIBITOR OF ACTIVATED BLOOD COAGULATION FACTOR X (FXA)

An object of the present invention is to provide a novel method for producing a compound, a salt thereof, or a hydrate of the compound or the salt, which is an FXa inhibitor. The object can be attained by a production method in which a production method via a compound represented by formula (1-1), etc., from a compound represented by the following formula (1-x), etc., is used for a method for producing a compound represented by the following formula (X), etc. [wherein X represents a halogen atom or the like, and R1 represents an optionally substituted phenyl group].

PROCESS FOR PRODUCING THIAZOLE DERIVATIVE

The present invention provides processes for producing a compound (5) based on the following reaction scheme. [F1]