Ruthenium-Catalyzed Mono-Selective C–H Methylation and d₃-Methylation of Arenes

[Image: see text] Site-selective installation of C–Me bonds remains a powerful and sought-after tool to alter the chemical and pharmacological properties of a molecule. Direct C–H functionalization provides an attractive means of achieving this transformation. Such protocols, however, typically utilize harsh conditions and hazardous methylating agents with poor applicability toward late-stage functionalization. Furthermore, highly monoselective methylation protocols remain scarce. Herein, we report an efficient monoselective, directed ortho-methylation of arenes using N,N,N-trimethylanilinium salts as noncarcinogenic, bench-stable methylating agents. We extend this protocol to d(3)-methylation in addition to the late-stage functionalization of pharmaceutically active compounds. Detailed kinetic studies indicate the rate-limiting in situ formation of MeI is integral to the observed reactivity

The ASTRO-H mission

The joint JAXA/NASA ASTRO-H mission is the sixth in a series of highly successful X-ray missions initiated by the Institute of Space and Astronautical Science (ISAS). ASTRO-H will investigate the physics of the high-energy universe by performing high-resolution, high-throughput spectroscopy with moderate angular resolution. ASTRO-H covers very wide energy range from 0.3 keV to 600 keV. ASTRO-H allows a combination of wide band X-ray spectroscopy (5-80 keV) provided by multilayer coating, focusing hard X-ray mirrors and hard X-ray imaging detectors, and high energy-resolution soft X-ray spectroscopy (0.3-12 keV) provided by thin-foil X-ray optics and a micro-calorimeter array. The mission will also carry an X-ray CCD camera as a focal plane detector for a soft X-ray telescope (0.4-12 keV) and a non-focusing soft gamma-ray detector (40-600 keV) . The micro-calorimeter system is developed by an international collaboration led by ISAS/JAXA and NASA. The simultaneous broad bandpass, coupled with high spectral resolution of ΔE ~7 eV provided by the micro-calorimeter will enable a wide variety of important science themes to be pursued