| 摘要 |
PROBLEM TO BE SOLVED: To obtain the subject tricyclic indole-2-carboxylic acid derivative that is useful as an intermediate for medicines or agrochemicals under mild conditions with reduced side-reactions by allowing a specific indole derivative to react with trialkyltin hydride or cyclizing the derivative with a Pd catalyst and reducing the product with samarium in the presence of iodine. SOLUTION: An indole derivative of formula I (R and R1 are each H, a protecting group of carboxyl; R5i is H, methyl; X is an alkyl, a halogen, cyano; X1 is Br, I) is allowed to react with a trialkyltin hydride, or cyclized with a Pd catalyst followed by the reduction with samarium in the presence of iodine to give a tricyclic indole-2-carboxylic acid derivative of formula II. According to this process, these reactions proceeds under mild conditions accompanied by reduced side-reactions to provide the objective compound that is useful as an intermediate for medicines and agrochemicals. |
