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Menezes, Reginaldo Ramos de; Santos, Alexandre Soares dos; Oestreicher, Enrique G.; Pinto, Gerson F.

doi:10.1023/a:1008899308479

Cited by 6 publications

(3 citation statements)

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“…1) would involve the (R)-enantiomer (via, e.g., the corresponding triflate), and as a result decided to investigate the use of other microorganisms. Several collections have become available in Brazil in recent years and as Candida guilliermondii, Aureobasidium pullulans, 3 Pichia pastoris, Pichia anomala 4 and Pichia angusta 5 have not been so used in microbial reductions, these were chosen as potential tools for the desired transformation. It is worth noting, however, that this empirical search is based upon our previous experience that the microorganism contains both pro-S and pro-R enzymes and under particular circumstances, a particular activity is preponderant.…”

Section: Introductionmentioning

confidence: 99%

Microbial reduction of ethyl 2-oxo-4-phenylbutyrate. Searching for R-enantioselectivity. New access to the enalapril like ACE inhibitors

Lacerda

Ribeiro²,

Leite³

et al. 2006

Tetrahedron: Asymmetry

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Section: Introductionmentioning

confidence: 99%

Microbial reduction of ethyl 2-oxo-4-phenylbutyrate. Searching for R-enantioselectivity. New access to the enalapril like ACE inhibitors

Lacerda

Ribeiro²,

Leite³

et al. 2006

Tetrahedron: Asymmetry

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“…Our research group has used both types of applications with good results. ,,,− However, the use of dehydrogenases in preparative applications requires effective processes of coenzyme regeneration since these cofactors are too expensive to be used as stoichiometric reagents. Moreover, since oxidation (or oxidative deamination) reactions are thermodynamically unfavorable, coenzyme regeneration by coupling to these reactions (strongly exergonic reduction reactions) drives the main reaction in the desired direction, making the whole system of coupled reactions to behave exergonically, allowing the main or desired reaction to proceed with high yields.…”

Section: Resultsmentioning

confidence: 99%

Thermodynamics and Kinetic Aspects Involved in the Enzymatic Resolution of (R,S)-3-Fluoroalanine in a Coupled System of Redox Reactions Catalyzed by Dehydrogenases

Gonçalves¹,

Antunes²,

Oestreicher³

2006

Org. Process Res. Dev.

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Two systems of redox enzymatic reactions were tested, looking forward to the preparation of (S)-3-fluoroalanine, a potent antibiotic, by kinetic resolution of rac-3-fluoroalanine. This starting material was the main substrate for the deaminative oxidation reaction catalyzed by L-alanine dehydrogenase (L-AlaDH) in the presence of NAD + . One system was formed by coupling this reaction (main reaction) to the reduction of 3-fluoropyruvate (a cascade system) produced in the main reaction catalyzed by L-lactate dehydrogenase (L-LDH) in the presence of NADH, also formed in the main reaction. This system, that was able to achieve 92% of conversion, allows the accumulation of NH 4 + , one of the secondary products of the main reaction. The other coupled redox system involved the coupling to the L-AlaDH reaction to the aminative reduction reaction of r-ketoglutarate in the presence of NADH and NH 4 + (both side products of the main reaction) catalyzed by Lglutamate dehydrogenase (L-GluDH), that allows accumulation of 3-fluoropyruvate. With this system, the extent of the reaction in the coupled system was only 22%. This big difference in the efficiency of both systems was identified as being the result of a different potency of the products that accumulates in both systems, acting as inhibitors of L-AlaDH. It was demonstrated that 3-fluoropyruvate is a much stronger inhibitor of L-AlaDH than NH 4 + . This fact, and not thermodynamic considerations, explains the results obtained with both systems.

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“…Este estudo que prossegue hoje na URI-Erechim 61 , foi parcialmente financiado pelo Programa PROCAD/CAPES e demonstrou ser possível a produção de alfaterpineol 62,63 (Figura 20). 65,66 . Uma vez que determinados fármacos utilizam beta-hidroxiácidos como intermediári-os quirais, a correta manipulação de microorganismos possibilitaria o acesso tanto à (R)-como à (S)-beta-hidroxiesteres.…”

Section: (Figura 17)unclassified

Interfaces com a indústria

Antunes¹

2005

Quím. Nova

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INTERFACES WITH THE INDUSTRY. Brazilian chemical industries face several problems regarding Research, Development and Innovation (RDI). The present paper shows that simple cooperation between chemical industries and university laboratories can be a way to overcome some of the present difficulties. The work carried out at LABOCAT has several industrial interfaces. It involves, among other areas of RDI, the development of anti-HIV-protease (and other virus-related-protease) drugs, the establishment of new (industrial) chemical processes and the implementation of industrial (biodiesel and related) plants. A model based on the present so called RHAE programme is proposed in which, parallel to the fellowship awards of this programme, financing participation of Brazilian Agencies would cover process development.Keywords: process development; pharmaceuticals; biotechnology. INTRODUÇÃOO Brasil tem problemas imensos e tudo ainda está por fazer. No caso da Indústria Química, nosso parque industrial não está à altura da dimensão econômica do País. Se, por um lado, fomos capazes de criar tecnologias para exploração de petróleo e para desenvolvimento do uso de outras formas de energia, por outro não fomos capazes de criar uma indústria de intermediários químicos avançados e de produtos finais (especialidades).Há necessidade premente de apoio governamental a indústrias brasileiras de intermediários e finais, particularmente, no que diz respeito à produção de APIs (ingredientes farmacêuticos ativos = princípios ativos dos medicamentos), já que quase a totalidade deles é importada. Recentemente, na questão das patentes do tenofovir diisoproxil fumarato (Viread ® ), efavirenz (Sustiva ® ) e ritonavir e lopivavir (Kaletra ® ) viu-se o grau de fragilidade e dependência externa de nosso país.Urge reequipar Universidades e Centros de Pesquisa (Públicos ou Privados), criar um sistema de pleno emprego de doutores em Química com aproveitamento imediato em indústrias e universidades. É preciso expandir o quadro e a remuneração dos bolsistas de produtividade do CNPq e, ao mesmo tempo, incentivar a interação universidade-indústria.O modelo RHAE (Programa de Recursos Humanos em Áreas Estratégicas -CNPq) é interessante para as indústrias em termos de apropriação de mão-de-obra, ao menos temporariamente, Porém, não há nele, ou relacionado a ele, um sistema que permita o financiamento para o projeto e sua posterior implementação em escala comercial, nem contra-partidas, para a Universidade, nos casos de parcerias com o setor privado.Da mesma maneira, a fixação do pesquisador na indústria, no período pós-projeto, deveria ser incentivada por mecanismos adicionais e/ou ao abrigo da chamada Lei da Inovação. A ênfase deverá ser sempre o apoio continuado e crescente, ao longo do tempo, à pesquisa como atividade sistêmica (e não pontual).O Laboratório de Catálise (LABOCAT) está envolvido no desenvolvimento de processos químicos e bioquímicos e procura atender as demandas industriais sem perder o foco de formação de recursos humanos, atividade-fim da...

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Cited by 6 publications

References 6 publications

Microbial reduction of ethyl 2-oxo-4-phenylbutyrate. Searching for R-enantioselectivity. New access to the enalapril like ACE inhibitors

Microbial reduction of ethyl 2-oxo-4-phenylbutyrate. Searching for R-enantioselectivity. New access to the enalapril like ACE inhibitors

Thermodynamics and Kinetic Aspects Involved in the Enzymatic Resolution of (R,S)-3-Fluoroalanine in a Coupled System of Redox Reactions Catalyzed by Dehydrogenases

Interfaces com a indústria

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