Process for producing 1-chlorocarbonyl-4-piperidinopiperidine or hydrochloride thereof
AssigneeKabushiki Kaisha Yakult Honsha
InventorHiroshi Hirota
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Abstract
The present invention provides a highly safe and easily operable process for producing 1-chlorocarbonyl-4-piperidinopiperidine or hydrochloride thereof in a high yield. Described specifically, the present invention relates to a process for producing 1-clorocarbonyl-4-piperidinopiperidine or hydrochloride thereof, which comprises reacting 4-piperidinopiperidine with a trialkylsilyl halide to obtain a 4-piperidinopiperidinyl trialkylsilyl, reacting it with a carbon dioxide gas to obtain a 4-piperidinopiperidinyl trialkylsilyl carbamate derivative, reacting the derivative with thionyl chloride or the like to obtain 1-chlorocarbonyl-4-piperidinopiperidine hydrochloride and optionally treating it with a strong base.
Claims1
A process for producing 1-chlorocarbonyl-4-piperidinopiperidine hydrochloride represented by the following formula (4):
- ##STR2## or 1-chlorocarbonyl-4-piperidinopiperidine represented by the following formula (5):
- ##STR3## which comprises reacting 4-piperidinopiperidine represented by the following formula (1):
- ##STR4## with a trialkylsilyl halide to obtain a 4-piperidinopiperidinyl trialkylsilyl represented by the following formula (2):
- ##STR5## wherein R.sup.1, R.sup.2 and R.sup.3 are the same or different and each independently represents a linear or branched C.sub.1-6 alkyl group;
- reacting the resulting compound with a carbon dioxide gas to obtain a 4-piperidinopiperidinyl trialkylsilyl carbamate derivative represented by the following formula (3):
- ##STR6## wherein R.sup.1, R.sup.2 and R.sup.3 have the same meanings as defined above;
- reacting the derivative with one or more substances selected from thionyl chloride, phosphorus trichloride, phosphorus pentachloride, oxalyl chloride and phosphoryl trichloride;
- and optionally reacting with a strong base.
Dependencies are inferred from the claim text.