The competitive muscarinic receptor antagonist fesoterodine is a congener of tolterodine and has better efficiency compared to tolterodine. In this study, we present an efficient synthesis of the fesoterodine intermediate 3-(3-diisopropylamino-1-phenylpropyl)-4-hydroxybenzaldehyde from ethyl benzoylacetate by Friedel-Crafts alkylation in the presence of an acid as a key reaction step. The synthesis is carried out by the reduction of the ketoester to a 1,3-diol, diisopropylamine substitution, and Friedel-Crafts alkylation, followed by reduction and chiral resolution.

Background: Little is known about the specific types of childhood trauma and their relationship to treatment-related issues in major depressive disorder (MDD). This study examined trauma experiences and treatment-related variables in outpatients with MDD at a psychiatric department of a university hospital in Korea. Methods: First, 75 outpatients with MDD were compared to medical outpatients without MDD matched by age, sex, income, and educational qualifications. Both groups completed the Life Stressor Checklist-Revised, which assesses comprehensive life events. Second, treatment-related variables and medication compliance measured by the Compliance Rating Scale were investigated for the two-year period after the initial assessment. Results: The MDD group had experienced a significantly higher number of lifetime traumas than the control group (p=0.003), including more frequent witnessing of family violence (p<0.001), adulthood physical assault by a family member (p<0.001), and childhood emotional abuse (CEA) (p<0.001). CEA was associated with early onset of the first depressive episode and premature termination of pharmacotherapy; childhood physical neglect was associated with premature termination and less time in therapy. Conclusion: Our findings support the important influence of childhood emotional trauma and its relationship to treatment retention.

N-Sulfonylformamidines were synthesized from N-sulfonylsulfonamides by reacting with p-toluenesulfonyl chloride (TsCl) and N,N -disubstituted formamides. In this reaction, it was expected that mixing TsCl with the N,N-disubstituted formamide would generate an iminium salt (Vilsmeier reagent). The reaction avoids the use of metal catalysts and hazardous reagents, and the desired N-sulfonylformamidines were obtained in 60% to quantitative yields.