855300-09-3Relevant articles and documents
Synthesis method of rivastigmine optical isomerization intermediate and (R)-rivastigmine
-
Paragraph 0074-0076; 0083-0085; 0092-0094; 0101-0103, (2020/01/25)
The invention provides a synthesis method of a rivastigmine optical isomerization intermediate and (R)-rivastigmine. The method comprises the following steps: carrying out an asymmetric reductive amination reaction on 3-nitromethyl ethyl formate acetophen
A method for preparing Rivastigmine citrate (by machine translation)
-
Paragraph 0039-0041, (2019/10/23)
The invention discloses a method for preparing Rivastigmine citrate, said method is to meta-hydroxy acetophenone, methyl ethyl carbamic chloride as the raw material in the isotope energy level transitions, alternately high and low frequency ultrasonic and
A General Catalytic Method for Highly Cost- and Atom-Efficient Nucleophilic Substitutions
Huy, Peter H.,Filbrich, Isabel
supporting information, p. 7410 - 7416 (2018/04/30)
A general formamide-catalyzed protocol for the efficient transformation of alcohols into alkyl chlorides, which is promoted by substoichiometric amounts (down to 34 mol %) of inexpensive trichlorotriazine (TCT), is introduced. This is the first example of a TCT-mediated dihydroxychlorination of an OH-containing substrate (e.g., alcohols and carboxylic acids) in which all three chlorine atoms of TCT are transferred to the starting material. The consequently enhanced atom economy facilitates a significantly improved waste balance (E-factors down to 4), cost efficiency, and scalability (>50 g). Furthermore, the current procedure is distinguished by high levels of functional-group compatibility and stereoselectivity, as only weakly acidic cyanuric acid is released as exclusive byproduct. Finally, a one-pot protocol for the preparation of amines, azides, ethers, and sulfides enabled the synthesis of the drug rivastigmine with twofold SN2 inversion, which demonstrates the high practical value of the presented method.