Pitavastatin → CID 86600714

HRID 1295199

反応式

HRID 1295199 の反応式
[CH:1]1[CH:2]=[CH:3][C:4]2[N:10]=[C:9]([CH:11]3[CH2:13][CH2:12]3)[C:8](/[CH:14]=[CH:15]/[C@@H:16]([OH:24])[CH2:17][C@@H:18]([OH:23])[CH2:19][C:20]([OH:22])=[O:21])=[C:7]([C:25]3[CH:26]=[CH:27][C:28]([F:31])=[CH:29][CH:30]=3)[C:5]=2[CH:6]=1.[Ca].[Na:33]>C(O)C.[OH-].[Na+]>[CH:1]1[CH:2]=[CH:3][C:4]2[N:10]=[C:9]([CH:11]3[CH2:13][CH2:12]3)[C:8](/[CH:14]=[CH:15]/[C@@H:16]([OH:24])[CH2:17][C@@H:18]([OH:23])[CH2:19][C:20]([OH:22])=[O:21])=[C:7]([C:25]3[CH:30]=[CH:29][C:28]([F:31])=[CH:27][CH:26]=3)[C:5]=2[CH:6]=1.[Na:33]

参加物

6

反応物 3

HCID 5282452PitavastatinHCID 5360545SodiumHCID 5460341Calcium

生成物 1

HCID 86600714CID 86600714

試薬・触媒・溶媒 2

HCID 702Ethanol溶媒HCID 14798Sodium Hydroxide溶媒2 回

実験手順

Pitavastatin, its calcium salt (2:1) and its lactone are disclosed in three related U.S. patents (U.S. Pat. Nos. 5,011,930 A, 5,856,336 A and 5,872,130 A). In the 930' patent, pitavastatin sodium is prepared by converting ethyl (E)-3,5-dihodroxy[4′-(4″-fluorophenyl)-2′-(I cyclopropyl)-quinolin-3′-yl]-hept enoate, to the sodium salt in accordance to Example 2 by using an aqueous solution of sodium hydroxide. The compound is dissolved in ethanol, to which an aqueous solution of sodium hydroxide is added. The resulting mixture is stirred and the ethanol is removed under reduced pressure. Water is then added, and the mixture is further extracted with ether. The aqueous layer is then lyophilized to obtain the final product, or the aqueous layer is weakly acidified with a dilute solution of hydrochloric acid. The acidified aqueous layer is then extracted with ether. After extraction, the ether layer is dried over magnesium sulphate. Then the ether is removed under reduced pressure to obtain the sodium salt. The '930 patent and its related patents do not disclose the procedure for preparing the calcium salt of pitavastatin, and do not disclose amorphous or crystalline forms of pitavastatin calcium as well.

後処理

  1. additionis added
  2. customthe ethanol is removed under reduced pressure
  3. additionWater is then added
  4. extractionthe mixture is further extracted with ether

出典と根拠

ORDレコード
ord-cce0c7b4f3af4e2682d4719ca1028037
出典データセット
uspto-grants-2007_07
特許番号
US07241800B2

関連ノート

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