Invention Grant
US08501967B2 Process for the preparation of enantiomerically pure 1-substituted-3-aminoalcohols
有权
用于制备对映体纯的1-取代-3-氨基醇的方法
- Patent Title: Process for the preparation of enantiomerically pure 1-substituted-3-aminoalcohols
- Patent Title (中): 用于制备对映体纯的1-取代-3-氨基醇的方法
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Application No.: US13560621Application Date: 2012-07-27
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Publication No.: US08501967B2Publication Date: 2013-08-06
- Inventor: Walter Brieden , Martin Clausen , John McGarrity , Hanspeter Mettler , Dominique Michel
- Applicant: Walter Brieden , Martin Clausen , John McGarrity , Hanspeter Mettler , Dominique Michel
- Applicant Address: CH Basel
- Assignee: Lonza AG
- Current Assignee: Lonza AG
- Current Assignee Address: CH Basel
- Agency: Hoffmann & Baron LLP
- Priority: EP05003657 20050221
- Main IPC: C07D333/22
- IPC: C07D333/22

Abstract:
A process for the preparation of N-monosubstituted β-aminoalcohol sulfonates of formula (1a), (1b): wherein R1 is C6-20-aryl or C4-12-heteroaryl, each optionally being substituted with one or more halogen atoms and/or one or more C1-4-alkyl or C1-4-alkoxy groups, R2 is C1-4-alkyl or C6-20-aryl, each aryl optionally being substituted with one or more halogen atoms and/or one or more C1-4-alkyl or C1-4-alkoxy groups, and wherein R3 is selected from the group consisting of C1-18-alkyl, C6-20-cycloalkyl, C6-20-aryl and C7-20-aralkyl residues; including a) reacting a methyl ketone, a primary amine, formaldehyde and a sulfonic acid, at a pressure above 1.5 bar, optionally in a organic solvent, said organic solvent which can include water to provide N-monosubstituted β-aminoketone sulfonates of formula (II): wherein R1, R2 and R3 are as defined above, and b) asymmetrically hydrogenating.
Public/Granted literature
- US20120316350A1 PROCESS FOR THE PREPARATION OF ENANTIOMERICALLY PURE 1-SUBSTITUTED-3-AMINOALCOHOLS Public/Granted day:2012-12-13
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