Benzimidazoles possess various bioactivities, such as anti-HIV-I, antineoplastic, antiproliferation, antiparasitic and so on, hence the synthetic methods of this class of compounds have attracted much attention. In order to provide some inspiration of better synthetic method design, in this review these methods reported during past five years will be firstly classified into three types according to the reaction intermediates, namely N-methene o-diaminobenzene (or N-methene-o-nitroaniline), N-acyl o-diaminobenzenes and arylamidine (aryl guanidine).
A scaleup route for a first-generation covalent KRAS G12C inhibitor ARS-2102 was devised, featuring an "early crosscoupling" strategy to construct the tetra-substituted atropisomeric biaryl scaffold. An iterative diastereomeric recrystallization enabled an effective chiral resolution of key intermediate 24. A global deprotection followed by chemoselective functionalization afforded ARS-2102 in excellent yield and diastereomeric enrichment. This chromatography-free sequence was successfully executed on kilogram scale.
It is a common challenge for the surgeon to detect pathological tissues and determine the resection margin during a minimally invasive surgery. In this study, we present a drop-in sensor probe based on the electrical bioimpedance spectroscopic technology, which can be grasped by a laparoscopic forceps and controlled by the surgeon to inspect suspicious tissue area conveniently. The probe is designed with an optimized electrode and a suitable shape specifically for Minimally Invasive Surgery (MIS). Subsequently, a series of ex vivo experiments are carried out with porcine liver tissue for feasibility validation. During the experiments, impedance measured at frequencies from 1 kHz to 2 MHz are collected on both normal tissues and water soaked tissue. In addition, classifiers based on discriminant analysis are developed. The result of the experiment indicate that the sensor probe can be used to measure the impedance of the tissue easily and the developed tissue classifier achieved accuracy of 80% and 100% respectively.
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