Improved Methodology for the Preparation of Chiral Amines
Improved Methodology for the Preparation of Chiral Amines
Improved Methodology for the Preparation of Chiral Amines
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OMe<br />
OMe<br />
O<br />
HN<br />
HN<br />
HN<br />
O 2 N<br />
71 % yield, 95 % ee<br />
75 % yield, 85 % ee<br />
92 % yield, 91 % ee<br />
HN<br />
OMe<br />
HN<br />
OMe<br />
HN<br />
OMe<br />
71 % yield, 83 % ee<br />
2<br />
60 % yield, 90 % ee<br />
73 % yield, 96 % ee<br />
Scheme 3.23. Asymmetric Reductive Amination System Developed by MacMillan<br />
3.4. Green Chemistry and Reductive Amination:<br />
3.4.1. Green Chemistry Basic principles.<br />
Reductive amination is a one pot process <strong>for</strong> chiral amine syn<strong>the</strong>sis. As described previously,<br />
it has many advantages compared to <strong>the</strong> o<strong>the</strong>r available methodologies. One <strong>of</strong> <strong>the</strong> significant<br />
advantages <strong>of</strong> this methodology is that it is considered an environmentally friendly process.<br />
To understand on which bases scientists made such assumption, we have first to know more<br />
about green chemistry and environmentally friendly process.<br />
It is widely acknowledged that <strong>the</strong>re is a growing need <strong>for</strong> more environmentally acceptable<br />
processes in <strong>the</strong> chemical industry and pharmaceutical industry. This trend has led to <strong>the</strong><br />
concept <strong>of</strong> ‘Green Chemistry’. [65]<br />
The new trend differs dramatically from <strong>the</strong> old traditional concepts focused only on process<br />
efficiency and chemical yield. The new trend assigns <strong>the</strong> economic value <strong>of</strong> <strong>the</strong> process<br />
depending on its ability to eliminate waste at source and avoid <strong>the</strong> use <strong>of</strong> toxic and/or<br />
73