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US 2006/0149058 A1Published application
Preparation of 2-(2-arylmorpholin-2-yl) ethanol derivatives and intermediates
AssigneeSanofi-Aventis
InventorsAlain Aulombard, Francoise Bernon, Sabrina Bonnefoy, Alain Burgos, Claude Cabos, Erice Lucas
Life of this patent
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Abstract
The invention relates to a process for the preparation of substituted 2-vinyl-2-arylmorpholine derivatives as described herein. This invention also relates to 2-vinyl-2-arylmorpholine derivatives as well as intermediates therefor.
Claims9
A process for the preparation of a compound, in the enantiomerically pure form, in the form of a mixture of diastereoisomers or in the racemic form, of formula:
- in which X represents a halogen atom and R1 represents a benzyl group, a tert-butyloxycarbonyl group or an α-methylbenzyl group, of its optional salts with inorganic or organic acids, is prepared by cyclization of a compound, in the enantiomerically pure form, in the form of a mixture of diastereoisomers or in the racemic form, of formula:
- in which X and R1 are as defined for a compound of formula (II), and, optionally, the compound of formula (II) thus obtained is converted to one of its salts.
A compound of formula:
- in which X represents a halogen atom and R1 represents an N-protecting group chosen from a benzyl group, a benzyloxycarbonyl group, a 1-chloroethyloxycarbonyl group, a tert-butyloxycarbonyl group or an α-methylbenzyl group, in the racemic form, in the enantiomerically pure form or in the form of a mixture of diastereoisomers, and its optional salts with inorganic or organic acids.
A compound of formula:
- in which X represents a halogen atom and R1 represents a benzyl group, a tert-butyloxycarbonyl group or an α-methylbenzyl group, in the racemic form, in the enantiomerically pure form or in the form of a mixture of diastereoisomers, and its optional salts with inorganic or organic acids.
A compound of formula:
- in which X represents a halogen atom and Hal represents a halogen atom.
Dependencies are inferred from the claim text.