Gamma-Aminobutyric Acid → Alendronic Acid

HRID 412674

반응식

HRID 412674 반응식
[P:1]([OH:4])([OH:3])[OH:2].[NH2:5][CH2:6][CH2:7][CH2:8][C:9]([OH:11])=O.P(Cl)(Cl)Cl>>[CH2:7]([CH2:6][NH2:5])[CH2:8][C:9]([P:1]([OH:4])([OH:3])=[O:2])([P:1]([OH:4])([OH:3])=[O:2])[OH:11]

참가 물질

4

반응물 3

HCID 119Gamma-Aminobutyric AcidHCID 24387Phosphorus trichlorideHCID 107909Phosphorous acid

생성물 1

HCID 2088Alendronic Acid

반응 조건

온도
70 °C

실험 절차

The mixture of 5 eq. phosphorous acid, 4-aminobutyric acid and morpholine. HCl is melted together until uniform solution is formed. The reaction mixture is cooled to about 70° C. and 2 eq. of PCl3 are carefully added. The mixture is heated for about 5.5 hours before the reaction mixture is hydrolyzed in aqueous acid at about 80° C. and alendronate is isolated from an ethanolic solution.

후처리

  1. customis formed
  2. temperatureThe mixture is heated for about 5.5 hours before the reaction mixture
  3. customis hydrolyzed in aqueous acid at about 80° C.

출처 및 근거

ORD 기록
ord-b3a0f7fd2bd7403f9357ce99aee0cb71
출처 데이터셋
uspto-grants-2003_05
특허 번호
US06562974B2

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