| 摘要 |
<p>NEW MATERIAL:A compound expressed by formula I [(X) is formula II, etc.; R1 is H, salt, protecting group or 1-4C alkyl; R2 is H or methyl; R3 is OH, methyl, etc.; R4 and R5 are H, methyl, halogen, etc.; R6 is 1-9C alkyl (substituted by a 1-9C alkyl, etc.), etc.]. EXAMPLE:13,14-Dihydro-15-keto-16R,S-methyl-prostaglandin D. USE:A sedative and hypnotic agent or central nervous system agent capable of exhibiting sleep inducing and sedative action by peripheral administration, such as oral administration, subcutaneous or intravenous injection. PREPARATION:Corey lactone expressed by formula 1 as a raw material is subjected to the Collins oxidation to provide an aldehyde expressed by formula 2, which is then reacted with dimethyl (2-oxoalkyl)phosphonate to afford an alpha,beta-unsaturated ketone expressed by formula 3. The resultant ketone is subsequently reduced to provide a saturated ketone expressed by formula 4, which is then subjected to ketanolization, etc., to afford the aimed compound expressed by formula 1.</p> |
