181289-33-8Relevant articles and documents
Synthesis and characterization of impurities of an anticonvulsant drug, Pregabalin
Sripathi, Somaiah,Somesetti, Narender Rao,Veeramalla, Raju,Challa, Nageswar Rao,Peddi, Srinivasa Rao,Karnati, Venugopal Reddy
, p. 266 - 275 (2010)
During the process development of Pregabalin 1, a known anticonvulsant drug, six potential impurities were identified in the final crude material ranging from 0.01 to 0.15% by LCMS. All six impurities were subsequently synthesized and characterized by IR, MS and NMR spectral data. Four of the six related substances are known as 4-isobutylpyrrolidin-2-one 6, 3-isobutylglutaric acid 2, (R)-(-)-3-carbamoylmethyl-5-methylhexanoic acid 5 and (R)-(-)-3-aminomethyl-5-methylhexanoic acid 8, whilst (S)-3-aminomethyl-5- methylhexanoic acid isobutyl ester 9 and (S)-3-aminomethyl-5-methylhexanoic acid isopropyl ester 10 are new compounds reported for the first time in our process. The present work describes the formation, synthesis and characterization of these impurities. ARKAT USA, Inc.
METHOD FOR PREPARING PREGABALIN INTERMEDIATE (R)-3-(CARBAMOYLMETHYL)-5-METHYLHEXANOIC ACID
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Paragraph 0039; 0041; 0043; 0045; 0047, (2021/04/23)
A method for preparing pregabalin chiral intermediate (R)-3-(carbamoylmethyl)-5-methylhexanoic acid by a biological enzyme method. In particular, the method comprises: reacting compound (I) 3-isobutylglutaric acid, as a raw material, with a nitrogen-conta
Method for synthesizing pregabalin midbody
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Paragraph 0022-0041, (2019/11/20)
The invention discloses a method for synthesizing a pregabalin midbody, and belongs to the technical field of medicine preparation. According to the method for synthesizing the pregabalin midbody, ammonium chloride, ammonium bicarbonate, ammonium carbonate, ammonium oxalate, ammonium formate, ammonium bromide, ammonium iodide, ammonium hydroxide, formamide, acetamide, hydrazine hydrate and other solid or liquid substances are used as an ammonia source, under the action of alkaline, (S)-3-(ethoxy-formyl methyl)-5-methyl caproic acid is subjected to a room temperature reaction, and pregabalin midbody (R)-3-(carbamyl methyl)-5-methyl caproic acid is generated. The method for synthesizing the pregabalin midbody is simple to operate, the pregabalin midbody can be obtained with high yield underordinary-pressure room temperature, the reaction condition is mild, economic and environmentally friendly, and the method for synthesizing the pregabalin midbody is suitable for industrial production.