Chemical Process Research and Development, Amgen Inc., Thousand Oaks, California 91320, USA.
J Org Chem. 2011 Dec 2;76(23):9841-4. doi: 10.1021/jo2015664. Epub 2011 Nov 8.
Chemoselective reduction of nitro groups in the presence of activated heteroaryl halides was achieved via catalytic hydrogenation with a commercially available sulfided platinum catalyst. The optimized conditions employ low temperature, pressure, and catalyst loading (<0.1 mol % Pt) to afford heteroaromatic amines with minimal hydrodehalogenation byproducts.
通过使用商业可得的硫化铂催化剂进行催化氢化,在活化杂芳基卤化物存在下实现了硝基的化学选择性还原。优化条件采用低温、低压和低催化剂负载量(<0.1 mol % Pt),以最小的氢卤化副产物得到杂芳族胺。