申请人:Hoge Stewart Garrett
公开号:US20050222464A1
公开(公告)日:2005-10-06
Materials and methods for preparing P-chirogenic monophospholanes and bisphospholanes are disclosed. The methods employ stereoselective cyclization to generate the phospholane rings followed by pyramidal inversion to access a variety of P-chirogenic phospholanes. When bound to transition metals such as rhodium, the disclosed P-chirogenic phospholanes may be used as catalysts in asymmetric synthesis of valuable pharmaceutical chemical entities, including pregabalin.
本文披露了制备P-手性单膦杂环和双膦杂环的材料和方法。该方法采用立体选择性环化来生成膦杂环,然后通过金字塔翻转来访问各种P-手性膦杂环。当与铑等过渡金属结合时,所披露的P-手性膦杂环可用作催化剂,在制备有价值的药物化学物质,包括pregabalin的不对称合成中使用。