| 摘要 |
PROBLEM TO BE SOLVED: To enable to produce the subject compound capable of being utilized as an intermediate for synthesizing an anti-HIV medicine, etc., by reacting a tetrahydroisoquinoline carboxylic acid derivative with a halogen compound and subsequently with a tertiary butylamine. SOLUTION: An N-(substituted oxycarbonyl)-1,2,3,4-tetrahydroxyisoquionline-3- carboxylic acid of formula I [R1 is C(CH3 )3 , CH2 ph] is reacted with a halide such as thionyl chloride, and the obtained N-carboxy-1,2,3,4- tetrahydroisoguinoline-3-carboxylic acid anhydride of formula II is reacted with tertiary butylamine of the formula: R2 -NH2 [R2 is C(CH3 )3 ] to obtain the 1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid tertiary butylamide of formula III. The compound of formula III can simply and efficiently be obtained in a state maintaining the optical purity. |
