N-Acetylthyroxine → Thyroxine

HRID 1388087

반응식

HRID 1388087 반응식
C([NH:4][C@H:5]([C:25]([OH:27])=[O:26])[CH2:6][C:7]1[CH:14]=[C:12]([I:13])[C:11]([O:15][C:16]2[CH:23]=[C:21]([I:22])[C:20]([OH:24])=[C:18]([I:19])[CH:17]=2)=[C:9]([I:10])[CH:8]=1)(=O)C>B([O-])([O-])[O-].CN(C=O)C>[NH2:4][C@H:5]([C:25]([OH:27])=[O:26])[CH2:6][C:7]1[CH:8]=[C:9]([I:10])[C:11]([O:15][C:16]2[CH:17]=[C:18]([I:19])[C:20]([OH:24])=[C:21]([I:22])[CH:23]=2)=[C:12]([I:13])[CH:14]=1

참가 물질

4

반응물 1

HCID 20638380N-Acetylthyroxine

생성물 1

HCID 5819Thyroxine

시약·촉매·용매 2

HCID 6228Dimethylformamide용매2회HCID 26574Borate용매

실험 절차

STI is dissolved in 50 ml of borate-saline buffer pH 8.5, to a concentration of 16 mg/ml (38 μmole). N-hydroxysuccinimide ester of N-acetyl thyroxine (378 μmole, 346 mg) is dissolved in 50 ml of DMF in a separate container. Aliquots (2 ml) of the active ester in DMF are added to the STI at 5 minute intervals until all the active ester has been added. The reaction mixture is stirred at room temperature for an additional 3.5 hours, then terminated by dialysis against 2 liters of aqueous triethylamine pH 11. Chromatography of the product on a Sephadex G-75 column (5×100 cm) equilibrated with aqueous triethylamine, pH 11 is then conducted to isolate thyroxine (T4) conjugated to soybean trypsin inhibitor from free T4. Fractions containing 1-2 molecules of thyroxine per molecule of protein are isolated as the preferred reagent. Higher substituted fractions were obtained, although operable, they were less preferable.

후처리

  1. additionhas been added
  2. customterminated by dialysis against 2 liters of aqueous triethylamine pH 11

출처 및 근거

ORD 기록
ord-afae8acb7d9b4e64846b696f9c55c639
출처 데이터셋
uspto-grants-1984_02
특허 번호
US04430263

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