86,559 research outputs found
REACTION BETWEEN CARBODIIMIDES AND CARBOXYLIC ACIDS: NEW “ONE-POT” PROCESSES FOR THE SYNTHESIS OF SMALL HETEROCYCLES OF BIOLOGICAL INTEREST
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A Mild, Efficient Approach for the Synthesis of 1,5-Disubstituted Hydantoins
No full textAn efficient and straightforward two-step procedure for the
synthesis of N-1 alkyl/aryl-substituted hydantoins was developed,
starting from easily available starting materials. The
procedure envisages a highly regiospecific domino condensation/
aza-Michael (nucleophilic substitution)/O->N acyl migration
between activated α,β-unsaturated carboxylic acids
or α-haloaryl acetic acids, respectively, and N-tert-butyl- or
N-tritylcarbodiimides, leading to the regioselective formation
of hydantoins bearing the tertiary alkylic substituent in the 3-position, followed by selective removal the substituent. This
process avoids the use of harsh reaction conditions and toxic
reagents and is high yielding. A detailed study of the influence
of the structure of the reactants on the reaction outcome
is presented. A wide variety of final products having a primary,
secondary, cyclic and aryl substituent at the N-1 position
were successfully synthesized by this method
Effectiveness and management of ponatinib as second-line treatment in chronic myeloid leukemia: an analysis from the monitoring registries of the Italian medicines agency (AIFA)
No full textManagement of chronic myeloid leukaemia patients treated with ponatinib in a real-life setting: A retrospective analysis from the monitoring registries of the Italian Medicines Agency (AIFA)
No full textReal-world data on daily practice management, treatment modifications and outcome of a large cohort of chronic myeloid leukaemia (CML) patients treated with ponatinib was performed through monitoring Registries of the Italian Medicines Agency (AIFA). Overall, 666 CML subjects were included in the ponatinib registry from February 2015 to December 2020 and were eligible for analysis: 515 in chronic phase (CP), 50 in accelerated phase (AP) and 101 in blast crisis (BC). Median age at baseline was 58.7 years with a predominance of male subjects (57.1%). The median time from diagnosis to start of ponatinib was 2.35 years: 259 (38.9%) subjects had received two previous lines of treatment, 260 (39.0%) three lines and 147 (22.1%) four or more lines. A molecular response [from major molecular response (MMR) to a score of ≤0.01% on the international reporting scale (IS)] was reported for 59% of patients out of 593 patients analysed. With a median follow-up of 14.4 months, 136 subjects (20.4%) required at least one dose reduction due to adverse events (AEs), whereas 309 patients (46.4%) required dose reduction in the absence of any evidence of side effects. Treatment discontinuation occurred in 261 patients (39%). This real-life analysis shows that dose reductions were made primarily as a precaution rather than due to the occurrence of adverse reactions
Regioselective multicomponent sequential synthesis of hydantoins
No full textThe development of new practical and green methods for the synthesis of small heterocycles is an
attractive area of research due to the well-known potential of heterocyclic small molecule scaffolds in the
drug discovery process. Herein we report a one-pot, three-component sequential procedure for the
synthesis of diversely 1,3,5- and 1,3,5,5-substituted hydantoins, in high yields and very mild conditions,
using readily accessible starting materials such as azides, iso(thio)cyanates and substituted α-halo-acetic
carboxylic acids. This methodology is especially convenient for the synthesis of spiro-hydantoins, which
are particularly interesting bioactive compounds in medicinal chemistry
The Influence of Grafting Degree on Chitosan-Graft-Branched Polyethylenimine Gene Vectors
No full textEffectiveness and management of ponatinib as second-line treatment in chronic myeloid leukemia: an analysis from the monitoring registries of the Italian medicines agency (AIFA)
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Influence of degree of grafting on transfection behavior of chitosan-graft-bPEI copolymers
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