OPTICALLY-ACTIVE 2-AMINO-PHOSPHONOALKANE ACID, OPTICALLY-ACTIVE 2-AMINOPHOSPHONOALKANE ACID SALT, AND HYDRATES OF THESE
First Claim
1. A method for producing an optically active 2-amino-phosphonoalkanoic acid salt, the method comprising:
- reacting, as a starting material, a DL-2-amino-phosphonoalkanoic acid represented by Formula (1) or a hydrate thereof with an optically active basic compound other than an optically active lysine, to give a diastereomeric salt mixture comprising;
a first salt (including a hydrate salt) between a D-2-amino-phosphonoalkanoic acid represented by Formula (1-1) and the optically active basic compound; and
a second salt (including a hydrate salt) between an L-2-amino-phosphonoalkanoic acid represented by Formula (1-2) and the optically active basic compound; and
subjecting the diastereomeric salt mixture to fractional crystallization to isolate one of the first and second diastereomeric salts, Formulae (1), (1-1), and (1-2) expressed as follows;
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Abstract
A novel compound has pharmacological activities comparable to those of Nahlsgen and is storable excellently stably. The compound can be produced by a method according to the present invention for producing an optically active 2-amino-phosphonoalkanoic acid salt. In the method, a starting material DL-2-amino-phosphonoalkanoic acid represented by Formula (1) or a hydrate thereof is reacted with an optically active basic compound other than an optically active lysine, to give a diastereomeric salt mixture including a first salt (including a hydrate salt) between a D-2-amino-phosphonoalkanoic acid represented by Formula (1-1) and the optically active basic compound, and a second salt (including a hydrate salt) between an L-2-amino-phosphonoalkanoic acid represented by Formula (1-2) and the optically active basic compound. The diastereomeric salt mixture is fractionally crystallized to isolate one of the first and second diastereomeric salts.
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9 Claims
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1. A method for producing an optically active 2-amino-phosphonoalkanoic acid salt, the method comprising:
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reacting, as a starting material, a DL-2-amino-phosphonoalkanoic acid represented by Formula (1) or a hydrate thereof with an optically active basic compound other than an optically active lysine, to give a diastereomeric salt mixture comprising; a first salt (including a hydrate salt) between a D-2-amino-phosphonoalkanoic acid represented by Formula (1-1) and the optically active basic compound; and a second salt (including a hydrate salt) between an L-2-amino-phosphonoalkanoic acid represented by Formula (1-2) and the optically active basic compound; and subjecting the diastereomeric salt mixture to fractional crystallization to isolate one of the first and second diastereomeric salts, Formulae (1), (1-1), and (1-2) expressed as follows; - View Dependent Claims (2, 3, 4, 7)
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5. A D-2-amino-phosphonoalkanoic acid salt or a hydrate of the salt, represented by Formula (1-1′
- -B);
- -B);
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6. An L-2-amino-phosphonoalkanoic acid salt or a hydrate of the salt, represented by Formula (1-2′
- -B);
- -B);
-
8. A D-2-amino-phosphonoalkanoic acid hydrate represented by Formula (1-1′
- );
- );
-
9. An L-2-amino-phosphonoalkanoic acid hydrate represented by Formula (1-2′
- );
- );
Specification