申请人:CHI Yonggui
公开号:US20080058548A1
公开(公告)日:2008-03-06
The present invention provides a method for the synthesis of β
2
-amino acids. The method also provides methods yielding α-substituted β-amino aldehydes and β-substituted γ-amino alcohols. The present method according to this invention allows for increased yield and easier purification using minimal chromatography or crystallization. The methods described herein are based on an aldehyde aminomethylation which involves a Mannich reaction between an aldehyde and a formaldehyde-derived N,O-acetal (iminium precursor) and a catalyst, such as, for example, L-proline or a pyrrolidine. The invention allows for large scale, commercial preparation of β
2
-amino acids.
本发明提供了一种合成β2-氨基酸的方法。该方法还提供了产生α-取代β-氨基醛和β-取代γ-氨基醇的方法。根据本发明的现有方法,可以使用最小的色谱或结晶实现增加产量和更容易的纯化。所述方法基于醛氨甲基化反应,包括醛和甲醛衍生的N,O-缩醛(亚胺前体)和催化剂之间的Mannich反应,例如L-脯氨酸或吡咯烷。本发明允许大规模、商业化制备β2-氨基酸。