The Experts below are selected from a list of 3204 Experts worldwide ranked by ideXlab platform

Shigeru Ohba - One of the best experts on this subject based on the ideXlab platform.

  • bimolecular solid state photoreactions in the adduct crystals of an Aromatic Nitro Compound with an Aromatic amine
    Tetrahedron Letters, 1994
    Co-Authors: Yoshikatsu Ito, Sadayuki Asaoka, Isao Saito, Shigeru Ohba
    Abstract:

    Abstract Solid-state as well as solution-state photochemistry of the donor-acceptor complexes derived from an Aromatic amine and an Aromatic Nitro Compound was investigated. Of the twelve adduct crystals studied, only three involving m-DNB as the acceptor (9-MC/m-DNB, 9-EC/m-DNB and DMAP/m-DNB) were found to be photoreactive in the solid state, producing photoredox products probably through hydrogen abstraction by the excited Nitro group. The FT-IR study has implicated that the NO 2 group of m-DNB may be interacting with the donor's amino group in the crystalline state.

Roger P Bakale - One of the best experts on this subject based on the ideXlab platform.

  • improved continuous flow processing benzimidazole ring formation via catalytic hydrogenation of an Aromatic Nitro Compound
    Organic Process Research & Development, 2014
    Co-Authors: Jian Chen, Katrin Przyuski, Renee C Roemmele, Roger P Bakale
    Abstract:

    In the development of a new route to bendamustine hydrochloride, the API in Treanda, the key benzimidazole intermediate 5 was generated via catalytic heterogeneous hydrogenation of an Aromatic Nitro Compound using a batch reactor. Because of safety concerns and a site limitation on hydrogenation at scale, a continuous flow hydrogenation for the reaction was investigated at lab scale using the commercially available H-Cube. The process was then scaled successfully, generating kilogram quantities on the H-Cube Midi. This flow process eliminated the safety concerns about the use of hydrogen gas and pyrophoric catalysts and also showed 1200-fold increase in space–time yield versus the batch processing.

Hans-jörg Martus - One of the best experts on this subject based on the ideXlab platform.

  • Genotoxicity assessment of the antiepileptic drug AMP397, an Ames-positive Aromatic Nitro Compound.
    Mutation Research Genetic Toxicology and Environmental Mutagenesis, 2002
    Co-Authors: Willi Suter, Andreas Hartmann, Franziska Poetter, Peter Sagelsdorff, Peter Hoffmann, Hans-jörg Martus
    Abstract:

    AMP397 is a novel antiepileptic agent and the first competitive AMPA antagonist with high receptor affinity, good in vivo potency, and oral activity. AMP397 has a structural alert (Aromatic Nitro group) and was mutagenic in Salmonella typhimurium strains TA97a, TA98 and TA100 without S9, but negative in the Nitroreductase-deficient strains TA98NR and TA100NR. The amino derivative of AMP397 was negative in wild-type strains TA98 and TA100. AMP397 was negative in a mouse lymphoma tk assay, which included a 24h treatment without S9. A weak micronucleus induction in vitro was found at the highest concentrations tested in V79 cells with S9. AMP397 was negative in the following in vivo studies, which included the maximum tolerated doses of 320mg/kg in mice and 2000mg/kg in rats: MutaMouse assay in colon and liver (5x320mg/kg) at three sampling times (3, 7 and 31 days after the last administration); DNA binding study in the liver of mice and rats after a single treatment with [14C]-AMP397; comet assay (1x2000mg/kg) in jejunum and liver of rats, sampling times 3 and 24h after administration; micronucleus test (2x320mg/kg) in the bone marrow of mice, sampling 24h after the second administration. Based on these results, it was concluded that AMP397 has no genotoxic potential in vivo. In particular, no genotoxic metabolite is formed in mammalian cells, and, if formed by intestinal bacteria, is unable to exert any genotoxic activity in the adjacent intestinal tissue. These data were considered to provide sufficient safety to initiate clinical development of the Compound.

Yoshikatsu Ito - One of the best experts on this subject based on the ideXlab platform.

  • bimolecular solid state photoreactions in the adduct crystals of an Aromatic Nitro Compound with an Aromatic amine
    Tetrahedron Letters, 1994
    Co-Authors: Yoshikatsu Ito, Sadayuki Asaoka, Isao Saito, Shigeru Ohba
    Abstract:

    Abstract Solid-state as well as solution-state photochemistry of the donor-acceptor complexes derived from an Aromatic amine and an Aromatic Nitro Compound was investigated. Of the twelve adduct crystals studied, only three involving m-DNB as the acceptor (9-MC/m-DNB, 9-EC/m-DNB and DMAP/m-DNB) were found to be photoreactive in the solid state, producing photoredox products probably through hydrogen abstraction by the excited Nitro group. The FT-IR study has implicated that the NO 2 group of m-DNB may be interacting with the donor's amino group in the crystalline state.

Jian Chen - One of the best experts on this subject based on the ideXlab platform.

  • improved continuous flow processing benzimidazole ring formation via catalytic hydrogenation of an Aromatic Nitro Compound
    Organic Process Research & Development, 2014
    Co-Authors: Jian Chen, Katrin Przyuski, Renee C Roemmele, Roger P Bakale
    Abstract:

    In the development of a new route to bendamustine hydrochloride, the API in Treanda, the key benzimidazole intermediate 5 was generated via catalytic heterogeneous hydrogenation of an Aromatic Nitro Compound using a batch reactor. Because of safety concerns and a site limitation on hydrogenation at scale, a continuous flow hydrogenation for the reaction was investigated at lab scale using the commercially available H-Cube. The process was then scaled successfully, generating kilogram quantities on the H-Cube Midi. This flow process eliminated the safety concerns about the use of hydrogen gas and pyrophoric catalysts and also showed 1200-fold increase in space–time yield versus the batch processing.