Dataset Information

Telescoped Continuous Flow Synthesis of Optically Active ?-Nitrobutyric Acids as Key Intermediates of Baclofen, Phenibut, and Fluorophenibut.

ABSTRACT: The two-step flow asymmetric synthesis of chiral ?-nitrobutyric acids as key intermediates of the GABA analogues baclofen, phenibut, and fluorophenibut is reported on a multigram scale. The telescoped process comprises an enantioselective Michael-type addition facilitated by a polystyrene-supported heterogeneous organocatalyst under neat conditions followed by in situ-generated performic acid-mediated aldehyde oxidation. Simple access to valuable optically active substances is provided with key advances in terms of productivity and sustainability compared to those of previous batch approaches.

SUBMITTER: Otvos SB

PROVIDER: S-EPMC7573919 | biostudies-literature | 2020 Oct

REPOSITORIES: biostudies-literature

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Telescoped Continuous Flow Synthesis of Optically Active γ-Nitrobutyric Acids as Key Intermediates of Baclofen, Phenibut, and Fluorophenibut.

Ötvös Sándor B SB Llanes Patricia P Pericàs Miquel A MA Kappe C Oliver CO

Organic letters 20201007 20

The two-step flow asymmetric synthesis of chiral γ-nitrobutyric acids as key intermediates of the GABA analogues baclofen, phenibut, and fluorophenibut is reported on a multigram scale. The telescoped process comprises an enantioselective Michael-type addition facilitated by a polystyrene-supported heterogeneous organocatalyst under neat conditions followed by <i>in situ</i>-generated performic acid-mediated aldehyde oxidation. Simple access to valuable optically active substances is provided wi ...[more]

PMID: 33026815

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Project description:AIM:To investigate the effects of continuous intrathecal baclofen (ITB) therapy in children with cerebral palsy (CP) and other neurological conditions. METHOD:This systematic review was conducted using standardized methodology, searching four electronic databases (PubMed, Embase, CINAHL, Cochrane Library) for relevant literature published between inception and September 2017. Included studies involved continuous ITB as an intervention and outcome measures relating to all International Classification of Functioning, Disability and Health: Children and Youth (ICF-CY) components. RESULTS:Thirty-three studies were identified, of which one, including 17 children with spastic CP, produced level II evidence, and the others, mainly non-controlled cohort studies, level IV and V. Outcomes at body function level were most frequently reported. Results suggest continuous ITB may be effective in reducing spasticity and dystonia in CP, as well as other neurological conditions, and may improve the ease of care and quality of life of children with CP, but the level of evidence is low. INTERPRETATION:Despite three decades of applying ITB in children and a relatively large number of studies investigating the treatment effects, a direct link has not yet been demonstrated because of the low scientific quality of the primary studies. Further investigation into the effects of continuous ITB at all levels of the ICF-CY is warranted. Although large, controlled trials may be difficult to realize, national and international collaborations may provide opportunities. Also, multicentre prospective cohort studies with a long-term follow-up, employing harmonized outcome measures, can offer prospects to expand our knowledge of the effects of continuous ITB therapy in children. WHAT THIS PAPER ADDS:There is low-level evidence for continuous intrathecal baclofen (ITB) in children with cerebral palsy. Continuous ITB is effective in reducing spasticity and dystonia in non-controlled cohort studies. Evaluation of individual goals and systematic assessment of long-term effects in large cohort studies are required.

Dataset Information

Telescoped Continuous Flow Synthesis of Optically Active ?-Nitrobutyric Acids as Key Intermediates of Baclofen, Phenibut, and Fluorophenibut.

Publications

Telescoped Continuous Flow Synthesis of Optically Active γ-Nitrobutyric Acids as Key Intermediates of Baclofen, Phenibut, and Fluorophenibut.

Similar Datasets

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