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US 6,646,150 B1Granted
Processes for producing (aminomethyl)trifluorocarbinol derivatives
AssigneeDainippon Pharmaceutical Co., Ltd.
InventorsFuminori Sato, Tomoki Omodani, Ryotaro Shiratake, Yasunao Inoue, Takashi Deguchi
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Abstract
The present invention provides a process for industrially producing (aminomethyl)trifluoromethylcarbinol derivatives, in particularly, optically active compounds thereof, which are useful as starting compounds for drugs such as protease inhibitors, etc.
Claims7
A process for producing an (aminomethyl)trifluoromethyl-carbinol derivative of the formula (I):
- wherein R1 is a group corresponding to the side chain of a natural or non-natural α-amino acid, R2 is a hydrogen atom or R21 (in which R21 is a protecting group for amino group having a carbonyl group at the binding site to the nitrogen atom), provided that when a functional group exists in R1, then such functional groups may optionally be protected,
- or an acid addition salt thereof,
- which comprises reducing a 5-hydroxy-5-trifluoromethyl-1,3-oxazolidine derivative of the formula (II):
- wherein R1 and R21 are as defined above,
- removing a protecting group for amino group R21 from the product to give a compound of the formula (I) wherein R2 is a hydrogen atom if necessary, then followed by converting the product into an acid addition salt thereof, if necessary.
2 more elements
Dependencies are inferred from the claim text.