Process for producing pyripyropene derivatives

摘要

Disclosed is a process for efficiently producing pyripyropene derivatives having acyloxy at the 1-position and 11-position and hydroxyl at the 7-position. The process comprises selectively acylating hydroxyl at the 1-position and 11-position of a compound represented by formula B1 through one to three steps with an acylating agent in the presence or absence of a base.;

主权项

1. A process for producing a compound C represented by formula C: wherein R represents a straight chain, branched chain, or cyclic C2-6 alkylcarbonyl, provided that, when the alkyl moiety in the alkylcarbonyl group is of a branched chain or cyclic type, then R represents C3-6 alkylcarbonyl, the process comprising: selectively acylating hydroxyl groups at the 1-position and 11-position of a compound B1 represented by formula B1: with an acylating agent in an amount of 2.0 to 5.0 equivalents based on the amount of the compound B1, through one to three steps in the presence or absence of a base, in an aprotic polar organic solvent selected from the group consisting of N,N-dimethylformamide, dimethylsulfoxide, N,N-dimethylacetamide, acetonitrile, N-methyl-2-pyrrolidinone, N-methyl-2-piperazinone and N,N-dimethyl-2-imidazolidinone, to obtain the compound C.