| 摘要 |
<p>PURPOSE:To produce the titled compound in high yield and stereroselectivity, in an industrial scale, with short reaction step, by using an allylglycine derivative as a starting raw material, reacting with N-bromosuccinimide, etc., removing the protecting group from the product, and hydrolyzing with an alkali. CONSTITUTION:The objective compound of formula III is produced in high purity by (1) reacting the allylglycine derivative of formula I (R<1> is amino-protecting group; R<2> is H or OH-protecting group) with N-bromosuccinimide or N-bromoacetamide or with bromine and pyridine in a solvent while passing mercury acetate, saline water and O2 gas successively to the reaction system, (2) eliminating the amino-protecting group of the bromolactone derivative of formula IIprepared by the step (1) in high yield and stereoselectivity, with an acid, (3) hydrolyzing with an alkali, and (4) eluting with ammonia water using an ion exchange resin. USE:Synthetic intermediate of anisomycin or acetylanisomycin of formula IV (R<3> is H or acetyl) known as a protozoacide and antiyeast antibiotic substance.</p> |
