Hydrochloric Acid → LY3020371 (hydrochloride)
반응식
C(OC([NH:8][C@@:9]1([C:33]([O:35]C(C)(C)C)=[O:34])[C@H:14]([CH2:15][S:16][C:17]2[CH:22]=[CH:21][C:20]([F:23])=[C:19]([F:24])[CH:18]=2)[C@@H:13]([OH:25])[C@@H:12]2[C@H:10]1[C@H:11]2[C:26]([O:28]C(C)(C)C)=[O:27])=O)(C)(C)C.[ClH:40]>ClCCl>[ClH:40].[NH2:8][C@@:9]1([C:33]([OH:35])=[O:34])[C@H:14]([CH2:15][S:16][C:17]2[CH:22]=[CH:21][C:20]([F:23])=[C:19]([F:24])[CH:18]=2)[C@@H:13]([OH:25])[C@@H:12]2[C@H:10]1[C@H:11]2[C:26]([OH:28])=[O:27]참가 물질
4
반응 조건
- 온도
- 70 °C
실험 절차
Di-tert-butyl (1S,2R,3S,4S,5R,6R)-2-[(tert-butoxycarbonyl)amino]-3-{[(3,4-difluorophenyl)sulfanyl]methyl}-4-hydroxybicyclo[3.1.0]hexane-2,6-dicarboxylate (0.58 g, 7.19 mmol) is weighed into a 100 mL round bottom with a stir bar. Hydrogen chloride (4N in dioxane, 33 mL, 132.0 mmol) is added. The mixture is warmed to 70° C. for 2 hours and then allowed to cool to ambient temperature. The solvent is removed under reduced pressure to give a residue. The residue is dissolve in dichloromethane (50 mL) and the solvent is removed under reduced pressure to give a residue. This is done three more times to give the title compound (567 mg, 1.43 mmol, 97% yield). MS (m/z): 360.0 (M+1).