930280-43-6

Upstream product

• 916982-10-0 3-isobutylglutarimide 
• 2627-86-3 (S)-1-phenyl-ethylamine 
• 75143-89-4 5-methyl-3-carboxymethylhexanoic acid 

Downstream Products

• 930280-44-7 {(S)-4-methyl-2-[((S)-1-phenylethylcarbamoyl)methyl]pentyl}carbamic acid methyl ester 
• 1310495-04-5 (S)-3-(aminomethyl)-5-methyl-N-((S)-1-phenylethyl)hexanamide 

Relevant academic research and scientific papers

Method for asymmetric preparation of (S)-3-aminomethyl-5-methylcaproic acid

The invention discloses a method for asymmetric preparation of (S)-3-aminomethyl-5-methylcaproic acid. The method is characterized by comprising the following four synthesis steps: with 3-isobutylglutaric acid as a raw material, subjecting 3-isobutylglutaric acid and a nitrogen-containing reagent to a ring-closure reaction; subjecting a reaction product and (S)-(+)-1-phenylethylamine to asymmetricring opening; carrying out Huffman rearrangement; and then carrying out amide hydrolysis so as to obtain (S)-3-aminomethyl-5-methylcaproic acid. Compared with the prior art, the method provided by the invention has the advantages of usage of cheap and easily available raw materials, short reaction steps, mild reaction conditions, and no usage of reagents easily leading to poisoning and explosion;the overall yield of method is as high as 72%; the purity of the product pregabalin is greater than 99%, and an ee value is greater than 99%; and the method has good application prospects in industrial large-scale production.

SYNTHESIS OF (S)-(+)-3-(AMINOMETHYL)-5-METHYL HEXANOIC ACID

Provided are syntheses of (S)-(+)-3-(aminomethyl)-5-methylhexanoic acid, (S)- Pregabalin via a chiral intermediate of the following formula (4) wherein Ar is a C6-10 aromatic group, R is a straight or branched C1-4 alkyl, ester, or carboxylic acid, and R1 is a straight or branched C1-5 alkyl, aralkyl, or substituted aralkyl.