148553-51-9Relevant articles and documents
PROCESS FOR THE PREPARATION OF GAMMA AMINO BUTYRIC ACIDS AND ANALOGS THEREOF
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, (2021/08/20)
The present invention relates to a process for the preparation of gamma aminobutyric acid derivatives of formula I, in particular pregabalin, baclofen and analogs thereof. Further, this process is comprised of preparation protocol for compounds of formula I, involving Michael addition and Beckmann rearrangement strategy.
Synthesis of (+/-)-Pregabalin and its novel lipophilic β-alkyl-substituted analogues from fatty chains
D'Oca, Caroline Da Ros Montes,Mass, Eduardo Bustos,Ongaratto, Renata Fontes,De Andrade, Arthur Motta,D'Oca, Marcelo G. Montes,Russowsky, Dennis
, p. 13230 - 13239 (2020/08/28)
In this work, were synthesized for the first time a series of new lipophilic β-alkyl substituted GABA derivatives from fatty alkyl chains. The synthesis of these GABA analogues was investigated by two different bicomponent approaches as a key step. The results showed low yields in the path from aliphatic nitroolefins and Meldrum's acid, whereas the Knoevenagel condensation between aliphatic aldehydes and Meldrum's acid afforded fatty alkylidenes in good yields (75-97%). These compounds were subsequently subjected to a conjugate addition reaction with nitromethane, resulting in the fatty Michael adducts (in 87-97% yields) which were in turn submitted to a one pot domino hydrolysis-decarboxylation, leading to the isolation of β-alkyl-substituted γ-nitro acids in good yields (78-92%). Finally, the reduction of the fatty γ-nitro acids allowed for the access to new lipophilic β-alkyl substituted GABA analogues, which were isolated in high yields (90-98%). The new methodology was also applied to the synthesis of antiepileptic drug (+/-)-Pregabalin, which was obtained after four steps in high overall yield. This journal is
Method for preparing 3-aminomethyl-5-methylcaproic acid
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Paragraph 0023; 0028-0029; 0031-0032; 0035-0036; 0039, (2020/07/13)
The invention relates to a method for preparing 3-aminomethyl-5-methylcaproic acid, belonging to the technical field of chemistry. According to the preparation method, 3-methyl formate-5-methylhexanoic acid is used as a raw material, and the target product 3-aminomethyl-5-methylcaproic acid can be prepared through two steps of reactions including ammonia ester exchange and reduction. The method has the beneficial effects of simple process route, high product purity of 99.0% or above, less three wastes, no toxic agent, mild reaction conditions and low cost, and is suitable for industrial production.
