Transition-Metal-Free Cross-Coupling Reactions in Dynamic Thin Films To Access Pyrimidine and Quinoxaline Analogues
The vortex fluidic device (VFD) is effective in modulating the synthesis of pyrimidine and quinoxaline-based compounds at room temperature and in high yield. The formation of the C–N bond occurs in the absence of a transition-metal catalyst, which avoids the contamination of the products with trace amounts of a transition metal. The systematic investigation of the operating parameters for the microfluidic platform in the confined operation mode established an optimum tilt angle of 45° for a 10 mm diameter borosilicate glass tube rotating at 5000 rpm.
Ho, Louisa A.,Raston, Colin L.,Stubbs, Keith A.
supporting information
p. 5957 - 5963
(2016/12/26)
Preparative access to medicinal chemistry related chiral alcohols using carbonyl reductase technology
Libraries of highly enantioenriched secondary alcohols in both enantiomeric forms were synthesised by enzymatic reduction of their parent ketones using selectAZyme carbonyl reductase (CRED) technology. Commercially available CREDs were able to reduce a range of substrate classes efficiently and with very high enantioselectivity. Matching substrate classes to small subsets of CREDs enabled the fast development of preparative bioreductions and the rapid generation of 100-1500 mg samples of chiral alcohols in typically >95% ee and the majority in ≥99.0% ee. The conditions for small scale synthesis were then scaled up to 0.5 kg to deliver one of the chiral alcohols, (S)-1-(4-bromophenyl)-2-chloroethanol, in 99.8% ee and 91% isolated yield.
Rowan, Andrew S.,Moody, Thomas S.,Howard, Roger M.,Underwood, Toby J.,Miskelly, Iain R.,He, Yanan,Wang, Bo
p. 1369 - 1381
(2013/12/04)
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