463967-83-1Relevant articles and documents
A Straightforward Deracemization of sec-Alcohols Combining Organocatalytic Oxidation and Biocatalytic Reduction
Liardo, Elisa,Ríos-Lombardía, Nicolás,Morís, Francisco,González-Sabín, Javier,Rebolledo, Francisca
, p. 3031 - 3035 (2018/06/27)
An efficient organocatalytic oxidation of racemic secondary alcohols, mediated by sodium hypochlorite (NaOCl) and 2-azaadamantane N-oxyl (AZADO), has been conveniently coupled with a highly stereoselective bioreduction of the intermediate ketone, catalyzed by ketoreductases, in aqueous medium. The potential of this one-pot two-step deracemization process has been proven by a large set of structurally different secondary alcohols. Reactions were carried out up to 100 mm final concentration enabling the preparation of enantiopure alcohols with very high isolated yields (up to 98 %). When the protocol was applied to the stereoisomeric rac/meso mixture of diols, these were obtained with very high enantiomeric excesses and diastereomeric ratios (95 % yield, >99 % ee, >99: 1 dr).
Modular, gold-catalyzed approach to the synthesis of lead-like piperazine scaffolds
James, Thomas,Simpson, Iain,Grant, J. Andrew,Sridharan, Visuvanathar,Nelson, Adam
supporting information, p. 6094 - 6097 (2014/01/06)
Ring-opening of cyclic sulfamidates with propargylic sulfonamides yielded substrates for a gold-catalyzed cyclization to yield tetrahydropyrazines. Manipulation of the tetrahydropyrazines, by reduction or using multicomponent reactions, yielded piperazine scaffolds in which substitution of the carbon atoms was varied. Such scaffolds may have value in the synthesis of novel screening compounds with lead-like molecular properties.
Development of a supply route for the synthesis of an iNOS inhibitor: Complications of the key SN2 reaction
Rassias, Geracimos,Hermitage, Stephen A.,Sanganee, Mahesh J.,Kincey, Peter M.,Smith, Neil M.,Andrews, Ian P.,Borrett, Gary T.,Slater, Graham R.
experimental part, p. 774 - 780 (2010/04/22)
The original medicinal chemistry synthesis of an iNOS inhibitor presented several challenges that had to be overcome in order to constitute a supply route suitable for operation on a multikilo scale. The key step in the synthesis is an SN2 reac
The first synthesis of optically active 1-substituted taurines
Xu, Jiaxi,Xu, Shu,Zhang, Qihan
, p. 466 - 471 (2007/10/03)
Optically active 1-substituted taurines, a type of important sulfur analogues of naturally occurring amino acids, and their N-benzyloxycarbonyl- protected derivatives were synthesized from the corresponding optically active β-amino secondary alcohols in t
COMBINATION THERAPY WITH INHIBITORS OF INDUCIBLE NITRIC OXIDE SYNTHASE AND ALKYLATING AGENTS
-
Page/Page column 87, (2010/02/11)
A combination therapy comprising administration of a carbamoylating chemotherapeutic agent in conjunction with administration of a selective iNOS inhibitor compound is disclosed. Optionally, resection and radiation therapy are provided with the therapeutic combination. A medicament comprising a carbamoylating chemotherapeutic agent and a selective iNOS inhibitor compound together with a pharmaceutically acceptable carrier is further disclosed. A kit comprising a carbamoylating chemotherapeutic agent and a selective iNOS inhibitor compound is further disclosed.
METHODS FOR TREATMENT AND PREVENTION OF GASTROINTESTINAL CONDITIONS
-
Page/Page column 81-82, (2010/02/06)
Therapeutic methods for the prevention ad treatment of conditions and diseases of the gastrointestinal tract involving an overproduction of nitric oxide by inducible nitric oxide synthase are described, the methods including administering to a subject in need thereof a therapeutically effective amount of a selective inhibitor of inducible nitric oxide synthase (iNOS). The methods also include the use of selective inhibitors of iNOs in combination with other therapeutic agents, including antimicrobial agents and antisecretory agents.
Agents and methods for treatment of cancer
-
, (2008/06/13)
Agents and methods for chemoprevention and treatment of neoplasia are described, the agents including a selective inhibitor of inducible nitric oxide synthase and a combination of a selective inhibitor of inducible nitric oxide synthase and an inhibitor of cylcooxygenase-2 in a pharmaceutical composition. The agents and methods are used for chemoprevention and treatment of neoplasia including colorectal cancer and other cancers affecting epithelial cells throughout the body. The agents can also be used to treat the fibrosis that occurs with radiation therapy, as well as adenomatous polyps, including those with familial adenomatous polyposis (FAP).
Amidino compound and salts thereof useful as nitric oxide synthase inhibitors
-
, (2008/06/13)
The present invention relates to S-[2-[(1-Iminoethyl)amino]ethyl]-2-methyl-L-cysteine, or a pharmaceutically acceptable salt thereof.