439585-11-2Relevant articles and documents
Preparation method of edoxaban
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, (2019/07/08)
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.
A novel, easy and mild preparation of sulfilimines from sulfoxides using the Burgess reagent
Raghavan, Sadagopan,Mustafa, Shaik,Rathore, Kailash
, p. 4256 - 4259 (2008/09/21)
A novel preparation of sulfilimines from the corresponding sulfoxides using the Burgess reagent is described. The reaction is general to dialkyl- and aryl alkyl sulfoxides and proceeds under mild conditions in benzene. A variety of protecting groups can be introduced on the nitrogen of the sulfilimine by choosing the appropriate Burgess reagent.
A novel, one-step method for the conversion of primary alcohols into carbamate-protected amines
Wood, Michael R.,Kim, June Y.,Books, Kathy M.
, p. 3887 - 3890 (2007/10/03)
A novel process for the one-step conversion of primary alcohols into carbamate-protected amines has been developed using a modified Burgess reagent. Although this letter mainly focuses on the conversion of alcohols into the corresponding Cbz-protected amines, the potential for extending this process to a wide range of carbamates has also been demonstrated. A detailed catalytic cycle has been proposed. While exploring the scope of this new reagent, an N-aryl piperidine to an N-aryl pyrrolidine rearrangement has been observed and rationalized.