Secondary Mannich Bases Via Trimethylsilyl Trifluoromethanesulphonate Promoted Addition Of Silyl Enol Ethers To Schiff Bases

A convenient route to N-aryl-β-aminoketones is reported involving addition of silyl enol ethers to Schiff bases activated with 15 mol % of trimethylsilyl trifluoromethanesulphonate.141053105

Diastereoselective Reduction Of Acyclic N-aryl-β-amino Ketones

A stereoselective route to anti- and syn-N-aryl-γ-amino alcohols is reported featuring the reduction of the corresponding β-amino ketones with Et3BHLi or Zn(BH4)2, respectively.41213121

Placebo Response of Non-Pharmacological and Pharmacological Trials in Major Depression: A Systematic Review and Meta-Analysis

Background: Although meta-analyses have shown that placebo responses are large in Major Depressive Disorder (MDD) trials; the placebo response of devices such as repetitive transcranial magnetic stimulation (rTMS) has not been systematically assessed. We proposed to assess placebo responses in two categories of MDD trials: pharmacological (antidepressant drugs) and non-pharmacological (device- rTMS) trials. Methodology/Principal Findings: We performed a systematic review and meta-analysis of the literature from April 2002 to April 2008, searching MEDLINE, Cochrane, Scielo and CRISP electronic databases and reference lists from retrieved studies and conference abstracts. We used the keywords placebo and depression and escitalopram for pharmacological studies; and transcranial magnetic stimulation and depression and sham for non-pharmacological studies. All randomized, double-blinded, placebo-controlled, parallel articles on major depressive disorder were included. Forty-one studies met our inclusion criteria - 29 in the rTMS arm and 12 in the escitalopram arm. We extracted the mean and standard values of depression scores in the placebo group of each study. Then, we calculated the pooled effect size for escitalopram and rTMS arm separately, using Cohen's d as the measure of effect size. We found that placebo response are large for both escitalopram (Cohen's d - random-effects model - 1.48; 95%C.I. 1.26 to 1.6) and rTMS studies (0.82; 95%C.I. 0.63 to 1). Exploratory analyses show that sham response is associated with refractoriness and with the use of rTMS as an add-on therapy, but not with age, gender and sham method utilized. Conclusions/Significance: We confirmed that placebo response in MDD is large regardless of the intervention and is associated with depression refractoriness and treatment combination (add-on rTMS studies). The magnitude of the placebo response seems to be related with study population and study design rather than the intervention itself

Addition of a chiral boron enolate to cyclic N-acyliminium ions. Stereocontrolled synthesis of the pyrrolizidine ring system

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SECONDARY MANNICH-BASES VIA TRIMETHYLSILYL TRIFLUOROMETHANESULFONATE PROMOTED ADDITION OF SILYL ENOL ETHERS TO SCHIFF-BASES

141053105

Addition of silylated carbon nucleophiles to iminium and cyclic N-acyliminium ions promoted by InCl3

InCl3 was used as Lewis acid in the addition of silyl enolates and allyltrimethylsilane to aromatic aldimines and cyclic N-acyliminium ions derived from 5-acetoxylactams affording beta -aminocarbonyl systems and allyl adducts, respectively, in reasonable to good yields. The diastereofacial selectivity of cyclic N-acyliminium ions was investigated. (C) 2000 Elsevier Science Ltd. All rights reserved.41519939994

Análise conformacional de compostos de Biginelli com atividade antineoplásica

Diidropirimidinonas são heterociclos com atividade antineoplásica conhecida. O monastrol e alguns análogos são exemplos. A análise conformacional representa uma etapa preliminar importante em estudos que visam correlacionar a estrutura do composto com sua atividade. Neste trabalho, descrevemos a análise conformacional do monastrol e diversos análogos por cálculo semi-empírico AM1 e ab initio HF/6-31G*. Quatro geometrias de equilíbrio foram encontradas (s-cis/ap, s-cis/sp, s-trans/ap e s-trans/sp), tendo como rotações internas importantes a do sistema carbonilado α,β-insaturado e a do grupo arila ligado ao heterociclo.</jats:p