| 摘要 |
A method for preparing the chiral (+/-) isomers of indole-2,3-dione-3-oxime derivatives of formula IIA or IIB, the method comprising: (I) reacting an 8-amino-1,2,3,4-tetrahydro-isoquinoline derivative with chloral hydrate and hydroxylamine hydrochloride to give an N-(1,2,3,4-tetrahydro-isoquinolin-8-yl)-2-hydroxyamino-acetamide derivative, (ii) adding sulphuric acid, (iii) reacting the 2,3-dioxo-2,3,6,7,8,9-hexahydro-1H-pyrrolo[3,2-h]isoquinoline derivative obtained from step (ii) with chiral (R) or (S) alpha-N,N-diBoc-aminoxy-gamma-butyrolactone to obtain the desired chiral end product.
|
