Improved Liquid and Mixed Metal Activation for Organic Synthesis

本申请是对EP/G 00272 X/1（2008年6月初审议）的修改后的立即重新提交，它得到了很高的评价，但优先级小组的资金不足。评审员对本申请中的领先科学的评论非常强烈（例如，“我见过的最新颖和令人耳目一新的提案”，“真正优秀的想法”，“杰出”等）但是资金环境不允许其支持。我们已经发现，催化液体镓可以用于高效的前所未有的金属活化，允许简化的有机金属化合物RM和金属氧化物的快速制备。该技术允许形成新的前所未有的空气稳定的芳基铝烷;直接使用金属混合物用于改进/有效的RX和氢和胺活化以提供Al-γ [HAl（NR 2）2]和[HAl（NR 2）Cl]以及DABCO稳定的空气稳定的有机金属化合物[（RnY 3-n）2（DABCO）]（Y = I，NR 2）。这些衍生试剂将用于快速通量（不对称）筛选FG-RCHO和亚胺的1，2-加成;不饱和酰基氰化物的1，4-加成;烯烃和炔烃的氢铝化及其随后在相关工艺中的应用。

This present application represents a revised immediate resubmission of EP/G00272X/1 (considered early June 2008) it was highly rated but insufficient funds were available to the prioritisation panel. Referee comments on the lead science in this application were very strong (e.g. 'most novel and refreshing proposal I haves seen', 'truly excellent ideas', 'outstanding', etc.) but the funding environment did not allow its support.We have found that catalytic liquid gallium can be used for highly efficient unprecedented metal activation allowing simplified rapid preparation of organometallics RM and metal hydrides. The technique allows formation of new unprecedented air-stable aryl alanes; direct use metal-mixtures for improved/efficient RX and hydrogen and amine activation to provide Al-hydrides [HAl(NR2)2] and [HAl(NR2)Cl] and the DABCO stabilized air-stable organometallics [(RnY3-n)2(DABCO)] (Y = I, NR2). These derived reagents are to be used in fast throughput (asymmetric) screening of 1,2-additions to FG-RCHO and imines; 1,4-additions to unsaturated acylcyanides; alkene and alkyne hydroalumination and their subsequent use in related processes.