A straightforward methodology for the enantioselective synthesis of 1,2-dihydrophthalazines dearomatization of phthalazines by anion-binding catalysis has been developed. The process involves the Mannich-type addition of silyl ketene acetals to generated -acylphthalazinium chlorides using a -leucine derived thiourea as a H-bond donor catalyst. Ensuing selective and high-yielding transformations provide appealing dihydro- and tetrahydro-phthalazines, phthalazones, and piperazic acid homologues, en route to biologically relevant molecules.
View Article and Find Full Text PDFEur J Surg Oncol
October 2023
Background: Pathologic complete response (pCR) after multimodal treatment for locally advanced rectal cancer (LARC) is used as surrogate marker of success as it is assumed to correlate with improved oncologic outcome. However, long-term oncologic data are scarce.
Methods: This retrospective, multicentre study updated the oncologic follow-up of prospectively collected data from the Spanish Rectal Cancer Project database.
Fetal movements (FM) are an important factor in the assessment of fetal health. However, there is currently no reliable way to monitor FM outside clinical environs. While extensive research has been carried out using accelerometer-based systems to monitor FM, the desired accuracy of detection is yet to be achieved.
View Article and Find Full Text PDFCatalysts generated by combinations of Pd(TFA) and pyridine-hydrazone ligands have allowed the asymmetric 1,2-addition of aryl boronic acids to N-carbamoyl (Cbz and Fmoc) protected glyoxylate-derived hydrazones, yielding α-aryl α-hydrazino esters/amides in high enantioselectivities. Subsequent removal of the carbamoyl moiety affords key building blocks en route to hydrazinopeptides, N-aminopeptides and peptidomimetics thereof.
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