cas 21172-43-0, Methanesulfonic acid 3-(3-trifluoroMethylphenyl)propyl ester

Articles about 21172-43-0Total 10 be found

Cinacalcet hydrochloride preparation method
The invention provides a cinacalcet hydrochloride preparation method, wherein the cinacalcet hydrochloride finished product is obtained by using 3-(3-trifluoromethylphenyl)propanol and (R)-(+)-1-(1-naphthyl)ethylamine as starting raw materials through two-step chemical reaction, one-step salt formation and two-step purification. According to the present invention, the method has characteristics ofsimple process, easily-available raw materials, economy and environmental protection, easily achieves industrialization, and can promote the economic and technological development of cinacalcet hydrochloride bulk drugs.
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Paragraph 0059-0061

(2019/07/04)

Method for preparing cinacalcet hydrochloride
The invention provides a method for preparing cinacalcet hydrochloride. The method comprises the following steps: with 3-(3-trifluoromethylphenyl)propanol shown as a formula I as a starting material,performing an acylation reaction on the starting material and methylsulfonyl chloride to obtain methylsulfonyl-3-(3-trifluoromethylphenyl) propyl ester shown as a formula II; in the presence of K2CO3,KI and ionic liquid 1-butyl-3-methylimidazolium trifluoromethanesulfonate, performing a substitution reaction on the methylsulfonyl-3-(3-trifluoromethylphenyl) propyl ester shown as the formula II and (R)-1-(1-naphthyl)ethylamine shown as a formula III to obtain a system containing a compound shown as a formula IV; performing a salt forming reaction on the compound shown as the formula IV and hydrochloric acid to obtain a target product, namely the cinacalcet hydrochloride. Through the addition of the trace KI and the ionic liquid 1-butyl-3-methylimidazolium trifluoromethanesulfonate in the substitution reaction in the step 2), the substitution reaction is speeded up, the yield of the product is increased and the purity of the product is improved.
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Paragraph 0031-0036

(2019/01/14)

Method for synthesizing calcimimetic cinacalcet hydrochloride
The invention provides a method for synthesizing calcimimetic cinacalcet hydrochloride; the method comprises the steps of preparing methylsulfonyl-3-(3-trifluoromethylphenyl)propionate; preparing (R)-(+)-1-(1-naphthyl)ethyltribenzyllamine; preparing N-((1R)-1-(1-napthyl)ethyl)-3-(3-(trifluoromethyl)phenyl)propyl-1-tribenzylamine; preparing N-((1R)-1-(1-napthyl)ethyl)-3-(3-(trifluoromethyl)phenyl)propylamine hydrochloride. The synthetic route of the method has the advantages of low price and easy access of materials, good operational simplicity, high yield and the like.
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Paragraph 0036; 0037; 0038; 0039

(2017/04/29)

Preparation method of high-purity m-trifluoromethyl phenylpropanol methanesulfonate
The invention belongs to the field of medicine preparation, and particularly relates to a preparation method of high-purity m-trifluoromethyl phenylpropanol methanesulfonate. The preparation method comprises the following steps of using m-trifluoromethyl phenylpropanol as the raw material, using methylsulfonyl chloride as an acylating agent, using triethylamine as an acid-binding agent, using dichloromethane as a solvent, and reacting; after reaction is finished, adding water to hydrolyze, standing and delaminating, drying and filtering an organic layer, and concentrating filtrate, so as to obtain the high-purity m-trifluoromethyl phenylpropanol methanesulfonate. The purity of the high-purity m-trifluoromethyl phenylpropanol methanesulfonate reaches 99.2% or above, the yield rate reaches 95% or above, and the prepared product can meet the requirement of medicine registration. The preparation method has the advantages that the production of impurities can be reduced by the reaction temperature, reaction time, and solvent removal by pressure-relief concentration, so as to improve the purity; the obtaining of raw materials is easy, the technology is reasonable, and the prepared sample can meet the requirement of medicine registration.
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Paragraph 0022; 0023; 0025; 0027

(2018/01/09)

Metal-Free Enantioselective Oxidative Arylation of Alkenes: Hypervalent-Iodine-Promoted Oxidative C?C Bond Formation
The enantioselective oxyarylation of (E)-6-aryl-1-silyloxylhex-3-ene was achieved using a lactate-based chiral hypervalent iodine(III) reagent in the presence of boron trifluoride diethyl etherate. The silyl ether promotes the oxidative cyclization, and enhances the enantioselectivity. In addition, the corresponding aminoarylation was achieved.
Shimogaki, Mio,Fujita, Morifumi,Sugimura, Takashi
p. 15797 - 15801
(2016/12/16)

PROCESS FOR PREPARING CINACALCET AND PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF
The resent invention rovides a novel rocess for re arin cinacalcet of formula I and pharmaceutically acceptable salts thereof and process of purification. The present invention also provides novel nitrogen protected synthetic intermediates useful in the process of the present invention. Further, the present invention provides a novel substituted carbamate impurity and process of preparation thereof.
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(2011/08/03)

PROCESS FOR THE PREPARATION OF CINACALCET AND SALTS THEREOF, AND INTERMEDIATES FOR USE IN THE PROCESS
There is provided a process for preparing a salt of the (R)- or (S)-isomer of 1- naphthylethylamine with mandelic acid or a derivative thereof, the process comprising reacting racemic 1-naphthylethylamine with mandelic acid or a derivative thereof to obtain the (R)- or (S)-isomer of 1-naphthylethylamine salt (III) with the acid. The salts also form an aspect of the present invention. There is also provided a salt of the (R)- or (S)-isomer of 1-naphthylethylamine with mandelic acid or a derivative thereof. There is also provided a process for preparing cinacalcet (I) or a salt thereof, the process comprising reacting an ester (II) with (R)-i-naphthylethylamine or a salt of (R)-i-naphthylethylamine and mandelic acid or a derivative thereof, to obtain cinacalcet, and optionally converting the cincalcet to a salt thereof.
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Page/Page column 19-20

(2010/09/18)

PROCESS FOR PREPARING CINACALCET AND PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF
The resent invention rovides a novel rocess for re arin cinacalcet of formula I and pharmaceutically acceptable salts thereof and process of purification. The present invention also provides novel nitrogen protected synthetic intermediates useful in the process of the present invention. Further, the present invention provides a novel substituted carbamate impurity and process of preparation thereof.
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Page/Page column 39

(2010/04/03)

Disubstituted imidazoles useful in the treatment of bacterial infections
Novel disubstituted imidazoles are disclosed which are useful in the treatment of bacterial infections, particularly through the inhibition of FAB I.
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(2008/06/13)