Penam crystals and process for producing the same
AssigneesOtsuka Chemical Co., Ltd., Taiho Pharmaceutical Co., Ltd.
InventorsYoshihisa Tokumaru, Akihiro Shimabayashi
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Abstract
The present invention provides novel 2α-methyl-2β-[(1,2,3-triazol-1-yl)methyl]penam-3α-carboxylic acid benzhydryl ester (TMPB)-acetone crystals for use in the production of 2α-methyl-2β-[(1,2,3-triazol-1-yl)methyl]penam-3α-carboxylic acid 1,1-dioxide benzhydryl ester (TAZB); a process for producing the TMPB-acetone crystals comprising the steps of (A) concentrating a TMPB-containing organic solvent solution, (B) dissolving the resulting concentrate in acetone, and (C) precipitating TMPB-acetone crystals from the acetone solution thus obtained; and a process for producing TAZB comprising the step of reacting the TMPB-acetone crystals with an oxidizing agent.
Claims10
2α-methyl-2β[(1,2,3-triazol-1-yl)methyl]penam-3α-carboxylic acid benzhydryl ester-acetone crystals.
A process for producing 2α-methyl-2β-[(1,2,3-triazol-1-yl)methyl]penam-3α-carboxylic acid benzhydryl ester-acetone crystals comprising the steps of:
- (A) concentrating a hydrophobic organic solvent solution containing 2α-methyl-2β-[(1,2,3-triazol-1-yl)methyl]penam-3α-carboxylic acid benzhydryl ester;
- (B) introducing the resulting concentrate to acetone;
- and
- (C) precipitating 2α-methyl-2β-[(1,2,3-triazol-1-yl)methyl]penam-3α-carboxylic acid benzhydryl ester-acetone crystals from the acetone solution thus obtained.
A process for producing 2α-methyl-2β-[(1,2,3-triazol-1-yl)methyl]penam-3αi-carboxylic acid 1,1-dioxide benzhydryl ester comprising the step of reacting in a solvent an oxidizing agent with 2α-methyl-2β-[(1,2,3-triazol-1-yl)methyl]penam-3α-carboxylic acid benzhydryl ester-acetone crystals.
A process for producing crystals of 2α-methyl-2β-[(1,2,3-triazol-1-yl)methyl]penam-3α-carboxylic acid benzhydryl ester comprising the step of de-acetonizing by maintaining the TMPB-acetone crystals under reduced pressure, 2α-methyl-2β-[(1,2,3-triazol-1-yl)methyl]penam-3α-carboxylic acid benzhydryl ester-acetone crystals.
A process for producing crystals of 2α-methyl-2β-[(1,2,3-triazol-1-yl)methyl]penam-3α-carboxylic acid benzhydryl ester comprising the steps of:
- (A) concentrating a hydrophobic organic solvent solution containing 2α-methyl-2β-[(1,2,3-triazol-1-yl)methyl]penam-3α-carboxylic acid benzhydryl ester;
- (B) introducing the resulting concentrate in acetone;
- (C) precipitating 2α-methyl-2β-[(1,2,3-triazol-1-yl)methyl]penam-3α-carboxylic acid benzhydryl ester-acetone crystals from the acetone solution thus obtained;
- and
- (D) de-acetonizing by maintaining the TMPB-acetone crystals under reduced pressure, the 2α-methyl-2β-[(1,2,3-triazol-1-yl)methyl]penam-3α-carboxylic acid benzhydryl ester-acetone crystals.
Dependencies are inferred from the claim text.