Sucrose → 2,3-Dihydroxybutanedioic Acid

HRID 1486412

Reaction equation

HRID 1486412 reaction equation
CCC1C=CC(CC[O:11]C2C=CC(CC3SC(=O)NC3=O)=CC=2)=NC=1.Cl.C(O)[C@H]1[O:33][C@H:32]([O:34][C@]2(CO)O[C@H](CO)[C@@H](O)[C@@H]2O)[C@H:31]([OH:46])[C@@H:30]([OH:47])[C@@H:29]1[OH:48]>>[C:32]([OH:33])(=[O:34])[CH:31]([CH:30]([C:29]([OH:48])=[O:11])[OH:47])[OH:46]

Participants

3

Reactant 2

HCID 5988SucroseHCID 60560Pioglitazone Hydrochloride

Product 1

HCID 8752,3-Dihydroxybutanedioic Acid

Procedure

Compound A (24.8 g), sucrose (Osaka-Toka. Co., Ltd., 28.7 g), crystalline cellulose (Avicel PH-101, Asahi Kasei Corporation, 8.0 g) and L-HPC (LH-31, Shin-Etsu Chemical Co., Ltd., 12.5 g) were thoroughly mixed to give a dusting powder. Tartaric acid crystal (Wako Pure Chemical Industries, Ltd.) was sieved with a round sieve to give tartaric acid crystal on 30 mesh (aperture 0.50 mm). The tartaric acid crystal (150 g) was fed into a centrifugal fluidized-bed granulator (CF-mini, Freund Corporation) and coated with the above-mentioned dusting powder while spraying an aqueous solution (6 w/v %) of hydroxypropylcellulose (HPC-SL, NIPPON SODA CO., LTD.). The obtained spherical granules were dried under reduced pressure in a constant temperature vacuum drying oven (DP43, YAMATO SCIENTIFIC CO., LTD.) at 40° C. for 16 hr to give granules at the range of 16-30 mesh (aperture 0.50-1.00 mm). The granules (450 mg) were filled in No. 0 gelatin capsules (Capsugel) to give capsules having the following composition per capsule.

Workup

  1. customto give a dusting powder
  2. filtrationTartaric acid crystal (Wako Pure Chemical Industries, Ltd.) was sieved with a round sieve

Sources & evidence

ORD record
ord-94bbc95cc03742638a7b723b0d48491a
Source dataset
uspto-grants-2016_08
Patent number
US09427434B2

Linked notes

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