二苯并[ b , f ][1,4]恶氮、二苯并[ b , f ] [1,4]硫氮和二苯并[ b , e ]氮杂衍生物与手性阳离子二胺钌催化剂的高效不对称氢化反应已被开发出来,得到多样的手性七元 N-杂环化合物,具有优异的结果(高达 99% 的产率和 99% 的 ee)。此外,发现催化剂抗衡阴离子在二苯并[ b,f ][1,4]噻氮和二苯并[ b,e ]衍生物的加氢反应中明显调节对映体选择性。
A highly efficient asymmetrichydrogenation of azepine/oxazepine-type seven-member cyclic imine hydrochlorides was successfully developed using Rh/bisphosphine-thiourea ligand ZhaoPhos, affording various chiral seven-member cyclic amines with full conversions, high yields, and excellent enantioselectivities (up to 96% yield, >99% ee). Additionally, this asymmetrichydrogenation can proceed well on
A class of pyrazole derivatives is described for use in treating p38 kinase medicated disorders. Compounds of particular interest are defined by Formula IA
wherein R
1
, R
2
, R
3
and R
4
are as described in the specification.