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US 2006/0069250 A1Published application
Synthesis by chiral diamine-mediated asymmetric alkylation
AssigneeJanssen Pharmaceutica NV
InventorsXiaohu Deng, Neelakandha Mani
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Abstract
Chiral synthesis from an achiral starting material by chiral diamine-mediated, such as sparteine-mediated, intermolecular asymmetric alkylation with a strained cyclic ether in the presence of a Lewis acid.
Claims47
A method for making a chiral alkylated derivative of a nitrogen-containing heterocycle, comprising:
- incorporating into a medium with an α-substitutable-N-heterocycle at least an organometalic compound, a chiral diamine, a strained cyclic ether, and a Lewis acid.
A method as in cliam 8, wherein said α-substitutable-N-heterocycle has its >NH member protected.
A method for making a chiral alkylated derivative of a nitrogen-containing heterocycle, comprising:
- step for forming a N-heterocycle-metal-chiral diamine complex.
Dependencies are inferred from the claim text.