These are isolated and fully characterized by melting/decomposition points, [alpha](D), elemental analysis, IR and NMR spectroscopy, and high-resolution mass spectrometry (HR-MS). Salts with BF(4), PF(6), SbF(6), and the weakly coordinating Al[OC(CF(3))(3)](4) anion were prepared. X-Ray crystal Structures of an enamine and of six iminium salts have been obtained and are described herein (Figs. 2 AZD1208 in vitro and 4-8, and Tables 2 and 7) and in a previous preliminary communication (Helv. Chim. Acta 2008, 91, 1999). According
to the NMR spectra (in CDCl(3), (D(6))DMSO, (D(6))acetone, or CD(3)OD; Table 1), the major isomers 4 of the iminium salts have (E)-configuration of the exocyclic N=C(1′) bond, but there are up to 11% of the (Z)-isomer present in these
solutions (Fig. 1). In all crystal structures, the iminium ions have (E)-configuration, and the conformation around the exocyclic N-C-C-O bond is synclinal-exo (cf. C and L), with one of the phenyl groups over the pyrrolidine ring, and the RO group over the pi-system. One of the meta-substituents (Me in 4b, CF(3) in 4c and 4e) on a 3,5-disubstituted phenyl group is also located in the space above the pi-system. DFT Calculations at various levels of theory (Tables 3-6) confirm Epigenetic inhibitor that the experimentally determined structures (cf. Fig. 10) are by far (up to 8.3 kcal/mol) the most stable ones. Implications of the results with respect to the mechanism of organocatalysis by diarylprolinol derivatives are discussed.”
“A high complete remission (CR) rate has been reported in newly diagnosed Philadelphia Roscovitine chromosome-positive
acute lymphoblastic leukemia (Ph+ALL) following imatinib-based therapy. However, the overall effect of imatinib on the outcomes of allogeneic hematopoietic stem cell transplantation (allo-HSCT) is undetermined. Between 2002 and 2005, 100 newly diagnosed adult patients with Ph+ALL were registered to a phase II study of imatinib-combined chemotherapy (Japan Adult Leukemia Study Group Ph+ALL202 study) and 97 patients achieved CR. We compared clinical outcomes of 51 patients who received allo-HSCT in their first CR (imatinib cohort) with those of 122 historical control patients in the pre-imatinib era (pre-imatinib cohort). The probability of overall survival at 3 years after allo-HSCT was 65% (95% confidence interval (CI), 49-78%) for the imatinib cohort and 44% (95% CI, 35-52%) for the pre-imatinib cohort. Multivariate analysis confirmed that this difference was statistically significant (adjusted hazard ratio, 0.44, P = 0.005). Favorable outcomes of the imatinib cohort were also observed for disease-free survival (P = 0.007) and relapse (P = 0.002), but not for non-relapse mortality (P = 0.265).