Diversity-oriented asymmetric synthesis of hapalosin: Construction of three small C9/C4/C3-modified hapalosin analogue libraries
- 化学化工－已发表论文 
A flexible approach to the beta-hydroxy gamma-amino acid residue (fragment C) of hapalosin has been developed on the basis of the the regio- and diastereoselective Grignard reaction. The method allows the introduction of different side chains at the C9 of hapalosin. Asymmetric syntheses of hapalosin (1a), 9- homohapalosin (1b), 9-i-butyl-hapalosin (1c), 8-epi-hapalosin (epi-1a), and three small libraries diversified at C9 (3-member, 1L(3)), C9/C4 (9-member, 1L(9)), or C9/C4/C3 (27-member, 1L(27)) have been produced using this method.