ABSTRACT: Strained aminomethyl-cycloalkanes are a recurrent scaffold in medicinal chemistry {due to|because of|as a result of|on account of|resulting from|as a consequence of} their {unique|distinctive|special|exclusive|exceptional|one of a kind} structural {features|attributes|functions|characteristics|capabilities|options} that give rise to a {range|variety} of biological properties. {Here|Right here}, we report a palladium-catalyzed enantioselective C(sp3)–H arylation of aminome-thyl-cyclopropanes and -cyclobutanes with aryl boronic acids. A {range|variety} of native tertiary alkylamine groups are {able to|in a position to} direct C–H cleavage and forge carbon-aryl bonds {on the|around the} strained cycloalkanes framework as single diastereomers and with {excellent|superb|outstanding|exceptional|great|fantastic} enantiomeric ratios. Cen-tral {to the|towards the|for the} {success|achievement|good results|accomplishment|results} of this {strategy|technique|method|approach|tactic} {is the|will be the|may be the|would be the|could be the|is definitely the} use of a {simple|easy|straightforward|basic|uncomplicated|very simple} N-acetyl amino acid ligand, which {not only|not just|not merely|not simply} controls the enantioselectivity {but also|but additionally|but in addition} promotes g-C–H activation of {over|more than} other pathways. Computational {analysis|evaluation} {of the|from the|in the|on the|with the|of your} cyclopalladation step {provides|offers|gives|supplies|delivers} an understanding of how enantioselective C–H cleavage {occurs|happens} and revealed distinct transition structures to our {previous|prior|earlier|preceding} {work|function|perform|operate} on enantioselective desymme-trization of N-iso-butyl tertiary alkylamines. This {straightforward|simple} and operationally {simple|easy|straightforward|basic|uncomplicated|very simple} {method|technique|approach|strategy|system|process} simplifies the {construction|building} of func-tionalized aminomethyl-strained cycloalkanes, which we {believe|think} will {find|discover|locate|uncover|come across|obtain} widespread use in academic and industrial settings relating {to the|towards the|for the} synthesis of biologically active {small|little|tiny|modest|smaller|compact} molecules. Eugenol acetate site Sulforaphane web PMID:23415682
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