Hydrochloric Acid → (RS)-Clopidogrel

HRID 1590780

反応式

HRID 1590780 の反応式
Cl.[S:2]1[CH:6]=[CH:5][CH:4]=[C:3]1[CH2:7][CH2:8][NH:9][CH:10]([C:15]1[CH:20]=[CH:19][CH:18]=[CH:17][C:16]=1[Cl:21])[C:11]([O:13][CH3:14])=[O:12].[CH2:22]=O>C(Cl)Cl>[S:2]1[C:3]2[CH2:7][CH2:8][N:9]([CH:10]([C:15]3[CH:20]=[CH:19][CH:18]=[CH:17][C:16]=3[Cl:21])[C:11]([O:13][CH3:14])=[O:12])[CH2:22][C:4]=2[CH:5]=[CH:6]1

参加物

5

反応物 3

HCID 313Hydrochloric AcidHCID 712FormaldehydeHCID 10223136Methyl [2-(2-thienyl)ethylamino](2-chlorophenyl)acetate

生成物 1

HCID 2806(RS)-Clopidogrel

試薬・触媒・溶媒 1

HCID 6344Dichloromethane溶媒

実験手順

35 g of the hydrochloride of racemic methyl alpha-(2-thienylethylamino)(2-chlorophenyl)acetate are suspended in 150 ml of a 30% (w/w) aqueous solution of formaldehyde. The mixture is kept at 50° C. for 2 hours and then poured, at about 20° C., into 200 ml of methylene chloride. The organic phase is concentrated and the residual oil is dissolved in 120 ml of isopropyl ether in which the hydrochloride is prepared as before; 29.5 g are obtained.

後処理

  1. concentrationThe organic phase is concentrated
  2. dissolutionthe residual oil is dissolved in 120 ml of isopropyl ether in which the hydrochloride
  3. customis prepared as before
  4. custom29.5 g are obtained

出典と根拠

ORDレコード
ord-f5c9992b4803468f97c3f790d71a0507
出典データセット
uspto-grants-1993_04
特許番号
US05204469

関連ノート

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