Search results for "Oxazepine"

Organocatalytic enantioselective Strecker reaction with seven-membered cyclic imines

2018

[EN] A highly enantioselective Strecker reaction with dibenzo[b,f][1,4]oxazepines has been described using a dihydroquinine-derived thiourea as organocatalyst. The reaction affords chiral 10,11-dihydrodibenzo[b,f][1,4] oxazepine 11-carbonitrile derivatives in excellent yields (up to 99%) and excellent enantioselectivities (up to 98%) under mild reaction conditions.

Catalytic Asymmetric Reactions Involving the Seven-Membered Cyclic Imine Moieties Present in Dibenzo[b,f][1,4]oxazepines

2017

The dibenzo[b,f][1,4]oxazepine scaffold is a privileged structure in medicinal chemistry that displays a wide variety of biological and pharmacological activities. However, catalytic asymmetric methodologies for the synthesis of chiral dibenzo[b,f][1,4]oxazepine derivatives are scarce in the literature. This microreview presents an overview of enantioselective reactions in which these cyclic seven-membered imines are used as electrophiles, including their substrate scope, limitations and application to the synthesis of related compounds.

Phase II Study of Taselisib (GDC-0032) in Combination with Fulvestrant in Patients with HER2-Negative, Hormone Receptor–Positive Advanced Breast Canc…

2018

AbstractPurpose: This single-arm, open-label phase II study evaluated the safety and efficacy of taselisib (GDC-0032) plus fulvestrant in postmenopausal women with locally advanced or metastatic HER2-negative, hormone receptor (HR)-positive breast cancer.Patients and Methods: Patients received 6-mg oral taselisib capsules daily plus intramuscular fulvestrant (500 mg) until disease progression or unacceptable toxicity. Tumor tissue (if available) was centrally evaluated for PIK3CA mutations. Adverse events (AE) were recorded using NCI-CTCAE v4.0. Tumor response was investigator-determined using RECIST v1.1.Results: Median treatment duration was 4.6 (range: 0.9–40.5) months. All patients expe…

Savoxepine: invalidation of an "atypical" neuroleptic response pattern predicted by animal models in an open clinical trial with schizophrenic patien…

1991

The new tetracyclic compound savoxepine exhibits potent antidopaminergic effects with preferential activity in the hippocampus as compared to striatum in rat brain. As a result of behavioural animal models and regional differences in dopamine receptor binding characteristics, it has been suggested to possess an "atypical" neuroleptic response pattern. In an open clinical trial, savoxepine was administered to 12 in-patients suffering from paranoid schizophrenia and schizophreniform disorder (DSM-III). Eight patients were treated with a stable dose of 0.5 mg per day throughout the study, while in the remaining patients higher doses up to 20 mg/day were administered. Mean total BPRS scores and…

Screening of oxazepine indole enantiomers by means of high performance liquid chromatography with imprinted polymer stationary phase.

2004

Chromatographic enantiomer separations of different oxazepine indole derivatives were performed using a molecularly imprinted polymer. A 5aR,12R,13S-trans-6,6-dimethyl-12,13-dihydro-6H-5a, 1 3-methanoindolo[2,1-b][1,3]naphthoxazepine-12-carboxamide enantiomerderivative was used as a template and the resultant polymer has shown enantiomer recognition for series of template related compounds. The mechanistic description of the chiral discrimination process is scrutinised, comparing the discrimination between the different conformations and substituents of the oxazepine indoles.

Synthesis of isoindolo[1,4]benzoxazinone and isoindolo[1,5]benzoxazepine: two new ring systems of pharmaceutical interest

2015

Abstract Two new ring systems, isoindolo[1,4]benzoxazinone and isoindolo[1,5]benzoxazepine, were conveniently synthesized through cyclization of suitably substituted isoindole derivatives. Some of the new compounds exhibited antiproliferative activity against a wide range of human tumor cell lines with GI 50 mean values at low micromolar level (3.72–5.13 μM).

Isoindolo[1,5]benzoxazepines as potential antitumor and/or antiviral agents

2013

Synthesis of Azole-Heterocycles as Potential Antitumor and/or Antiviral Agents

2014

Isoindolo[1,5]benzoxazepine as Potential Antitumor and/or Antiviral Agents

2013

CCDC 1847752: Experimental Crystal Structure Determination

2018

Related Article: Carles Lluna‐Galán, Gonzalo Blay, Isabel Fernández, M. Carmen Muñoz, José R. Pedro, Carlos Vila|2018|Adv.Synth.Catal.|360|3662|doi:10.1002/adsc.201800754