Process for producing optically active 3-amino...

Organic compounds -- part of the class 532-570 series – Organic compounds – Heterocyclic carbon compounds containing a hetero ring...

Reexamination Certificate

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Reexamination Certificate

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08030501

ABSTRACT:
Aiming at production of an optically active 3-amino nitrogen-containing compound which is useful as an intermediate in synthesis of medicines and pesticides, in particular, an optically active 1-protected-3-aminopyrrolidine derivative, from an inexpensive and readily available raw material by a process which is efficient and can be practiced industrially, an optically active 3-amino nitrogen-containing compound is produced by performing a reaction of an optically active 3-substituted nitrogen-containing compound with ammonia, methylamine, ethylamine or dimethylamine in the presence of water. In addition, a 1-protected-3-aminopyrrolidine derivative is produced by performing a reaction of an optically active 1-protected-3-(sulfonyloxy)pyrrolidine derivative with ammonia, methylamine, ethylamine, or dimethylamine in the presence of methanol, ethanol, n-propanol, or isopropanol under a pressure of less than 30 barr.

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Cesare et al. (J. Med. Chem. 1992, 35, 4205-4213.
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Vapor pressure of ethanol, which is available from the CRC Handbook of Chemistry and Physics, 44th ed—(years 1962-1963).
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International Search Report in PCT/JP2007/064406 dated Oct. 9, 2007.
Sanchez et al., J. Med. Chem. 35:1764-1773 (1992).

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