89580-42-7

Usage

Uses

Used in Pharmaceutical Industry:
4-Piperidinone, 3-bromo-1-methyl-, hydrobromide is used as a synthetic intermediate for the development of new drugs. Its unique structure allows for the creation of a wide range of pharmaceutical compounds, contributing to the advancement of medicinal chemistry.
Used in Agrochemical Industry:
In the agrochemical sector, 4-Piperidinone, 3-bromo-1-methyl-, hydrobromide is utilized as a precursor in the synthesis of agrochemicals. Its properties make it suitable for the development of innovative agricultural products, such as pesticides and herbicides, to improve crop protection and yield.

Upstream product

• 1445-73-4 1-Methyl-4-piperidone 

Downstream Products

• 143150-92-9 2-Bromo-5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]-pyridine 
• 720720-96-7 5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxylic acid hydrochloric acid salt 
• 480449-70-5 edoxaban 
• 480449-71-6 [14C]-Edoxaban tosylate 

Relevant academic research and scientific papers

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.

Preparation method of edoxaban

The invention relates to a new preparation route and a new method for a p-toluenesulfonic acid edoxaban hydrate and intermediates thereof. The new method comprises the steps that a high-reactivity compound 109A4x is prepared; a compound 109C6x is prepared by using a new synthesizing method; new compounds 109E8-01, 109E9x and 109T7-01 are prepared; the p-toluenesulfonic acid edoxaban hydrate is prepared by using the intermediates. By using the new method and the new route, the reaction step of copious cooling is omitted, and dangerous elemental sulfur, high-risk n-butyllithium and high-risk azides are prevented from being used. In a word, by means of the method, the p-toluenesulfonic acid edoxaban hydrate and the key intermediates thereof are more easily and safely prepared at a lower coston an industrialization scale.