- HETEROCYCLIC COMPOUND
-
The present invention provides a heterocyclic compound having a HDAC inhibitory action, and useful for the treatment of central nervous system diseases including neurodegenerative disease, and the like, and a medicament comprising the compound. The present invention relates to a compound represented by the formula (I) wherein each symbol is as defined in the specification, or a salt thereof.
- -
-
Paragraph 0477
(2019/02/15)
-
- Method for preparing beta arylamine
-
The invention discloses a method for preparing beta arylamine. The method includes mixing an aziridine compound, halogenated aromatic hydrocarbon, an oxidizing agent, a reducing agent and an organic solvent to obtain a mixed solution and obtaining the beta arylamine after reaction. The oxidizing agent is at least one of a mixture of nickel iodide and bipyridine, a mixture of nickel chloride dimethoxyethane and bipyridine and 2,2'-bipyridinium nickel iodide. The reducing agent is at least one of zinc powder, manganese powder, iron powder, cobalt powder, titanium powder, calcium powder and tetrakis(dimethylamino)ethylene. The halogenated aromatic hydrocarbon is at least one of the chlorinated aromatic hydrocarbon, the brominated aromatic hydrocarbon and aryl iodide. An organometallic reagentis not required, the preparation process is simple and reliable and high in yield, and the aziridine compound is wide in selection range.
- -
-
Paragraph 0051
(2019/01/14)
-
- Synthesis of β-fluoroamines by Lewis base catalyzed hydrofluorination of aziridines
-
Lewis base catalysis promotes the in situ generation of amine-HF reagents from benzoyl fluoride and a non-nucleophilic alcohol. The hydrofluorination of aziridines to provide β-fluoroamines using this latent HF source is described. This protocol displays a broad scope with respect to aziridine substitution and N-protecting groups. Examples of regio- and diastereoselective ring opening to access medicinally relevant β-fluoroamine building blocks are presented.
- Kalow, Julia A.,Schmitt, Dana E.,Doyle, Abigail G.
-
experimental part
p. 4177 - 4183
(2012/06/18)
-
- Hexahydro-5-imino-1,4-1,4-thiazepine derivatives as inhibitors of nitric oxide synthases
-
Disclosed herein are compounds of Formula I and pharmaceutically acceptable salts thereof which have been found useful in the treatment of nitric oxide synthase mediated diseases and disorders, including neurodegenerative disorders, disorders of gastrointestinal motility and inflammation. These diseases and disorders include hypotension, septic shock, toxic shock syndrome, hemodialysis, IL-2 therapy such as in in cancer patients, cachexia, immunosuppression such as in transplant therapy, autoimmune and/or inflammatory indications including sunburn, eczema or psoriasis and respiratory conditions such as bronchitis, asthma, oxidant-induced lung injury and acute respiratory distress (ARDS), glomerulonephritis, restenosis, inflammatory sequelae of viral infections, myocarditis, heart failure, atherosclerosis, osteoarthritis, rheumatoid arthritis, septic arthritis, chronic or inflammatory bowel disease, ulcerative colitis, Crohn's disease, systemic lupus erythematosis (SLE), ocular conditions such as ocular hypertension, retinitis and uveitis, type 1 diabetes, insulin-dependent diabetes mellitus and cystic fibrosis.
- -
-
-
- Base-promoted elaboration of aziridines
-
The base-promoted isomerization of aziridines to allyl amines is still an almost unknown reaction. However, the use of superbasic reagents has shown to be able to promote a regio- and stereoselective conversion of monocyclic and bicyclic sulfonyl aziridin
- Mordini, Alessandro,Russo, Francesco,Valacchi, Michela,Zani, Lorenzo,Degl'Innocenti, Alessandro,Reginato, Gianna
-
p. 7153 - 7163
(2007/10/03)
-
- Asymmetric Catalysis by Vitamin B12: The Isomerization of Achiral Aziridines to Optically Active Allylic Amines
-
Achiral N-acylaziridines are isomerized to optically active N-acyl-allylamines in ee's of up to 95percent by catalytic amounts of cob(I)alamin in MeOH.
- Zhang, Zhong da,Scheffold, Rolf
-
p. 2602 - 2615
(2007/10/02)
-