Hydrochloric Acid → Perindopril

HRID 273480노트

반응식

HRID 273480 반응식
[CH2:1]([O:3][C:4]([C@@H:6]([NH:10][C@H:11]([C:13]([OH:15])=O)[CH3:12])[CH2:7][CH2:8][CH3:9])=[O:5])[CH3:2].Cl.P(Cl)(Cl)(Cl)(Cl)Cl.[CH3:23][CH2:24][CH2:25][CH2:26][CH2:27][CH3:28]>>[CH3:9][CH2:8][CH2:7][C@H:6]([NH:10][C@H:11]([C:13]([N:10]1[C@H:6]([C:4]([OH:5])=[O:3])[CH2:7][C@H:24]2[C@@H:25]1[CH2:26][CH2:27][CH2:28][CH2:23]2)=[O:15])[CH3:12])[C:4]([O:3][CH2:1][CH3:2])=[O:5]

참가 물질

5

반응물 4

HCID 313Hydrochloric AcidHCID 8058HexaneHCID 24819Phosphorus pentachlorideHCID 10015159(2S)-2-[[(2S)-1-ethoxy-1-oxopentan-2-yl]amino]propanoic acid

생성물 1

HCID 107807Perindopril

실험 절차

To a slurry of N-[1-(S)-ethoxycarbonyl-1-butyl]-(S)-alanine (1.5 g, 0.0069 moles, as obtained in Step-IV, Method-I and Step-II, Method-II) in n-hexane (10 ml) was purged dry hydrogen chloride gas at 25-30° C. under agitation. To this was added finely ground phosphorous pentachloride (1.8 g, 0.0086 moles) in four lots, each after an interval of 10 mns. After the complete addition the reaction mixture was agitated for 1.5 hrs. The solid precipitated was filtered, washed with hexane to give 1.88 g of the title compound (I).

후처리

  1. additionAfter the complete addition the reaction mixture
  2. customThe solid precipitated
  3. filtrationwas filtered
  4. washwashed with hexane

출처 및 근거

ORD 기록
ord-8af06c45750f4697a90f36c85d15776d
출처 데이터셋
uspto-grants-2008_11
특허 번호
US07456296B2

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